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(2Z,6E)-farnesylphosphoryl-beta-D-ribofuranose + FAD
(2Z,6E)-farnesylphosphoryl-D-beta-D-erythro-pentofuranosid-2-ulose + FADH2
-
oxidation reaction calyzed by decaprenylphospho-beta-D-ribofuranose 2-oxidase DprE1
-
?
trans,octacis-decaprenylphospho-beta-D-ribofuranose + FAD
trans,octacis-decaprenylphospho-beta-D-erythro-pentofuranosid-2-ulose + FADH2
trans,octacis-decaprenylphospho-beta-D-ribofuranose + O2 + FAD
trans,octacis-decaprenylphospho-beta-D-erythro-pentofuranosid-2-ulose + H2O2 + FADH2
trans,octacis-decaprenylphospho-beta-D-ribofuranose + resazurin + FAD
trans,octacis-decaprenylphospho-beta-D-erythro-pentofuranosid-2-ulose + resorufin + FADH2
additional information
?
-
trans,octacis-decaprenylphospho-beta-D-ribofuranose + FAD
trans,octacis-decaprenylphospho-beta-D-erythro-pentofuranosid-2-ulose + FADH2
-
-
-
-
?
trans,octacis-decaprenylphospho-beta-D-ribofuranose + FAD
trans,octacis-decaprenylphospho-beta-D-erythro-pentofuranosid-2-ulose + FADH2
-
-
-
?
trans,octacis-decaprenylphospho-beta-D-ribofuranose + FAD
trans,octacis-decaprenylphospho-beta-D-erythro-pentofuranosid-2-ulose + FADH2
-
-
-
-
?
trans,octacis-decaprenylphospho-beta-D-ribofuranose + FAD
trans,octacis-decaprenylphospho-beta-D-erythro-pentofuranosid-2-ulose + FADH2
-
-
-
?
trans,octacis-decaprenylphospho-beta-D-ribofuranose + FAD
trans,octacis-decaprenylphospho-beta-D-erythro-pentofuranosid-2-ulose + FADH2
-
-
-
-
?
trans,octacis-decaprenylphospho-beta-D-ribofuranose + FAD
trans,octacis-decaprenylphospho-beta-D-erythro-pentofuranosid-2-ulose + FADH2
-
-
-
?
trans,octacis-decaprenylphospho-beta-D-ribofuranose + FAD
trans,octacis-decaprenylphospho-beta-D-erythro-pentofuranosid-2-ulose + FADH2
-
-
-
?
trans,octacis-decaprenylphospho-beta-D-ribofuranose + FAD
trans,octacis-decaprenylphospho-beta-D-erythro-pentofuranosid-2-ulose + FADH2
-
-
-
?
trans,octacis-decaprenylphospho-beta-D-ribofuranose + FAD
trans,octacis-decaprenylphospho-beta-D-erythro-pentofuranosid-2-ulose + FADH2
-
-
-
?
trans,octacis-decaprenylphospho-beta-D-ribofuranose + FAD
trans,octacis-decaprenylphospho-beta-D-erythro-pentofuranosid-2-ulose + FADH2
-
-
-
?
trans,octacis-decaprenylphospho-beta-D-ribofuranose + FAD
trans,octacis-decaprenylphospho-beta-D-erythro-pentofuranosid-2-ulose + FADH2
-
-
-
?
trans,octacis-decaprenylphospho-beta-D-ribofuranose + FAD
trans,octacis-decaprenylphospho-beta-D-erythro-pentofuranosid-2-ulose + FADH2
-
oxidation reaction catalyzed by decaprenylphospho-beta-D-ribofuranose 2-oxidase DprE1
-
?
trans,octacis-decaprenylphospho-beta-D-ribofuranose + FAD
trans,octacis-decaprenylphospho-beta-D-erythro-pentofuranosid-2-ulose + FADH2
-
-
-
?
trans,octacis-decaprenylphospho-beta-D-ribofuranose + O2 + FAD
trans,octacis-decaprenylphospho-beta-D-erythro-pentofuranosid-2-ulose + H2O2 + FADH2
-
-
-
?
trans,octacis-decaprenylphospho-beta-D-ribofuranose + O2 + FAD
trans,octacis-decaprenylphospho-beta-D-erythro-pentofuranosid-2-ulose + H2O2 + FADH2
-
-
-
?
trans,octacis-decaprenylphospho-beta-D-ribofuranose + resazurin + FAD
trans,octacis-decaprenylphospho-beta-D-erythro-pentofuranosid-2-ulose + resorufin + FADH2
-
-
-
?
trans,octacis-decaprenylphospho-beta-D-ribofuranose + resazurin + FAD
trans,octacis-decaprenylphospho-beta-D-erythro-pentofuranosid-2-ulose + resorufin + FADH2
-
-
-
?
additional information
?
-
decaprenylphospho-beta-D-ribofuranose 2-oxidase DprE1 and decaprenylphospho-beta-D-erythro-pentofuranosid-2-ulose 2-reductase DprE2 together catalyze the epimerization of decaprenylphosphoryl-beta-D-ribofuranose to decaprenylphosphoryl-beta-D-arabinofuranose. Neither protein individually is sufficient to support the activity
-
-
?
additional information
?
-
-
the enzyme can use synthetic electron acceptors such as 2,6-dichlorophenolindophenol with good efficiency
-
-
?
additional information
?
-
decaprenylphospho-beta-D-ribofuranose 2-oxidase DprE1 and decaprenylphospho-beta-D-erythro-pentofuranosid-2-ulose 2-reductase DprE2 together catalyze the epimerization of decaprenylphosphoryl-beta-D-ribofuranose to decaprenylphosphoryl-beta-D-arabinofuranose. Neither protein individually is sufficient to support the activity
-
-
?
additional information
?
-
decaprenylphosphoryl-beta-D-ribofuranose 2'-epimerase is constituted of decaprenylphospho-beta-D-ribofuranose 2-oxidase DprE1 and decaprenylphospho-beta-D-erythro-pentofuranosid-2-ulose 2-reductase DprE2 that together catalyze the epimerization of decaprenylphosphoryl-beta-D-ribofuranose to decaprenylphosphoryl-beta-D-arabinofuranose
-
-
?
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(3,4-dihydroisoquinolin-2(1H)-yl)[1-[5-(1H-pyrrol-1-yl)-1,3,4-thiadiazol-2-yl]piperidin-4-yl]methanone
-
(4-(2-methoxyethyl)piperazin-1-yl)(6-methyl-7-nitro-5-(trifluoromethyl)benzo[d]thiazol-2-yl)methanone
-
(4-benzylpiperazin-1-yl)[1-[5-(1H-pyrrol-1-yl)-1,3,4-thiadiazol-2-yl]piperidin-4-yl]methanone
-
(4-methylpiperidin-1-yl)[1-[5-(1H-pyrrol-1-yl)-1,3,4-thiadiazol-2-yl]piperidin-4-yl]methanone
-
(5-chloro-1-methyl-1H-pyrazol-4-yl)(3-endo-3-((5-fluoro-1H-indazol-3-yl)amino)-8-azabicyclo[3.2.1]oct-8-yl)methanone
-
(5-chloro-1-methyl-1H-pyrazol-4-yl)(4-((2-methoxyquinolin-4-yl)amino)piperidin-1-yl)methanone
-
(5-chloro-1-methyl-1H-pyrazol-4-yl)(4-((5-fluoro-1H-indazol-3-yl)amino)piperidin-1-yl)methanone
-
(5-chloro-1-methyl-1H-pyrazol-4-yl)(4-(cinnolin-4-ylamino)-piperidin-1-yl)methanone
-
(6-methyl-7-nitro-5-(trifluoromethyl)benzo[d]thiazol-2-yl)(piperidin-1-yl)methanone
-
(S)-(2-(6-methyl-7-nitro-5-(trifluoromethyl)benzo[d]thiazol-2-yl)-4,5-dihydrooxazol-4-yl)(pyrrolidin-1-yl)methanone
-
(S)-(2-(7-nitro-5-(trifluoromethyl)benzo[d]thiazol-2-yl)-4,5-dihydrooxazol-4-yl)(pyrrolidin-1-yl)methanone
-
(S)-7-nitro-2-(1-oxo-1-(pyrrolidin-1-yl)propan-2-ylcarbamoyl)-5-(trifluoromethyl)benzo[d]thiazole 3-oxide
-
(S)-N-(3-hydroxy-1-oxo-1-(pyrrolidin-1-yl)propan-2-yl)-6-methyl-7-nitro-5-(trifluoromethyl)benzo[d]thiazole-2-carboxamide
-
(S)-N-(4-hydroxy-1-oxo-1-(piperidin-1-yl)butan-2-yl)-6-methyl-7-nitro-5-(trifluoromethyl)benzo[d]thiazole-2-carboxamide
-
1,3-dimethyl-5-((3-(trifluoromethyl)benzylamino)methyl)-1Hpyrazolo[3,4-b]pyridin-6(7H)-one
1-(6-methoxy-3-methyl-1-phenyl-1H-pyrazolo[3,4-b]pyridin-5-yl)-N-(3-(trifluoromethyl)benzyl)methanamine
1-methyl-2,4,7-trinitroxanthone
mutations C387S and C387G confer resistance to 1-methyl-2,4,7-trinitroxanthone
1-[(4-tert-butylphenyl)methyl]-3-nitro-1H-1,2,4-triazole
-
-
1-[1-[5-(1H-pyrrol-1-yl)-1,3,4-thiadiazol-2-yl]piperidine-4-carbonyl]piperidine-4-carboxylic acid
-
2-(4,5-dihydrooxazol-2-yl)-7-nitro-5-(trifluoromethyl)benzo[d]thiazole 3-oxide
-
2-(4-(2-methoxyethyl)piperazine-1-carbonyl)-7-nitro-5-(trifluoromethyl)benzo[d]thiazole 3-oxide
-
2-(4-butylpiperazin-1-yl)-8-(1H-pyrrol-1-yl)-6-(trifluoromethyl)-4H-1,3-benzothiazin-4-one
PyrBTZ03
2-(6-methyl-7-nitro-5-(trifluoromethyl)benzo[d]thiazol-2-yl)-4,5-dihydrooxazole
-
2-(7-nitro-5-(trifluoromethyl)benzo[d]thiazol-2-yl)-4,5-dihydrooxazole
-
2-(methoxymethyl)-7-nitro-5-(trifluoromethyl)benzo[d]thiazole
-
2-(piperidine-1-carbonyl)-5-(trifluoromethyl)benzo[d]thiazol-7-ylboronic acid
-
2-(piperidine-1-carbonyl)-5-(trifluoromethyl)benzo[d]thiazole-7-carbonitrile
-
2-(piperidine-1-carbonyl)-5-(trifluoromethyl)benzo[d]thiazole-7-carboxylic acid
-
2-[(2S)-2-methyl-1,4-dioxa-8-azaspiro[4,5]dec-8-yl]-8-(1H-pyrrol-1-yl)-6-(trifluoromethyl)-4H-1,3-benzothiazin-4-one
PyrBTZ01
2-[(2S)-2-methyl-1,4-dioxa-8-azaspiro[4,5]dec-8-yl]-8-nitro-6-(trifluoromethyl)-4H-1,3-benzothiazin-4-one
BTZ043
2-[(2S)-2-methyl-1,4-dioxa-8-azaspiro[4.5]dec-8-yl]-8-nitro-6-(trifluoromethyl)-4H-1,3-benzothiazin-4-one
2-[(2S)-2-methyl-1,4-dioxa-8-azaspiro[4.5]decan-8-yl]-8-nitro-6-(trifluoromethyl)-4H-1,3-benzothiazin-4-one
2-[4-(cyclohexylmethyl)piperazin-1-yl]-8-(1H-pyrrol-1-yl)-6-(trifluoromethyl)-4H-1,3-benzothiazin-4-one
PyrBTZ02
2-[4-(cyclohexylmethyl)piperazin-1-yl]-8-(2,5-dimethyl-1H-pyrrol-1-yl)-6-(trifluoromethyl)-4H-1,3-benzothiazin-4-one
PyrBTZ04
2-[4-(cyclohexylmethyl)piperazin-1-yl]-8-nitro-6-(trifluoromethyl)-4H-1,3-benzothiazin-4-one
3,7-dimethyl-1-phenyl-5-((3-(trifluoromethyl)benzylamino)-methyl)-1H-pyrazolo[3,4-b]pyridin-6(7H)-one
3-(((3-methyl-6-oxo-1-phenyl-6,7-dihydro-1H-pyrazolo[3,4-b]-pyridin-5-yl)methylamino)methyl)benzonitrile
3-(2-(piperidine-1-carbonyl)-5-(trifluoromethyl)benzo[d]thiazol-7-yl)-1,2,3-oxadiazol-3-ium-5-olate
-
3-cyclopropyl-1-phenyl-5-(((6-(trifluoromethyl)pyridin-2-yl)-methylamino)methyl)-1H-pyrazolo[3,4-b]pyridin-6(7H)-one
3-cyclopropyl-1-phenyl-5-((3-(trifluoromethyl)benzylamino)-methyl)-1H-pyrazolo[3,4-b]pyridin-6(7H)-one
3-cyclopropyl-5-(((3-methyl-6-(trifluoromethyl)pyridin-2-yl)-methylamino)methyl)-1-phenyl-1H-pyrazolo[3,4-b]pyridin-6(7H)-one
3-cyclopropyl-5-((2-fluoro-3-(trifluoromethyl)benzylamino)-methyl)-1-phenyl-1H-pyrazolo[3,4-b]pyridin-6(7H)-one
3-cyclopropyl-5-((2-fluoro-5-(trifluoromethyl)benzylamino)-methyl)-1-phenyl-1H-pyrazolo[3,4-b]pyridin-6(7H)-one
3-cyclopropyl-5-((2-methyl-5-(trifluoromethyl)benzylamino)-methyl)-1-phenyl-1H-pyrazolo[3,4-b]pyridin-6(7H)-one
3-isopropyl-5-((2-methyl-5-(trifluoromethyl)benzylamino)-methyl)-1-phenyl-1H-pyrazolo[3,4-b]pyridin-6(7H)-one
3-methyl-1-(pyridin-2-yl)-5-((3-(trifluoromethyl)benzylamino)-methyl)-1H-pyrazolo[3,4-b]pyridin-6(7H)-one
3-methyl-1-p-tolyl-5-((3-(trifluoromethyl)benzylamino)methyl)-1H-pyrazolo[3,4-b]pyridin-6(7H)-one
3-methyl-1-phenyl-5-((3-(trifluoromethyl)benzylamino)methyl)-1H-pyrazolo[3,4-b]pyridin-6(7H)-one
3-methyl-1-phenyl-5-((7-(trifluoromethyl)-3,4-dihydroisoquinolin-2(1H)-yl)methyl)-1H-pyrazolo[3,4-b]pyridin-6(7H)-one
3-methyl-5-((2-methyl-5-(trifluoromethyl)benzylamino)methyl)-1-phenyl-1H-pyrazolo[3,4-b]pyridin-6(7H)-one
3-methyl-5-((3-methylbenzylamino)methyl)-1-phenyl-1Hpyrazolo[3,4-b]pyridin-6(7H)-one
3-methyl-5-((methyl(3-(trifluoromethyl)benzyl)amino)methyl)-1-phenyl-1H-pyrazolo[3,4-b]pyridin-6(7H)-one
3-methyl-6-oxo-1-phenyl-N-(3-(trifluoromethyl)benzyl)-6,7-dihydro-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
3-nitro-N-[(1R)-1-phenylethyl]-5-(trifluoromethyl)benzamide
3-nitroso-N-[(1R)-1-phenylethyl]-5-(trifluoromethyl)benzamide
benzothiazinone-derived inhibitor, binding includes a covalent link to conserved Cys387, and trifluoromethyl group is a second key determinant of interaction with the enzyme
3-{[(4-methoxyphenyl)methyl]amino}-6-(trifluoromethyl)quinoxaline-2-carboxylic acid
97% inhibition at 0.04 mM
4-(((1R,3R,5S)-8-((4,5-dimethylisoxazol-3-yl)carbonyl)-8-azabicyclo[3.2.1]octan-3-yl)amino)-6,7-difluoroquinolin-2(1H)-one
-
4-(((1R,3R,5S)-8-((5-chloro-1-methyl-1H-pyrazol-4-yl)carbonyl)-8-azabicyclo[3.2.1]octan-3-yl)amino)-1-methyl-1,8-naphthyridin-2(1H)-one
-
4-(((1R,3R,5S)-8-((5-chloro-1-methyl-1H-pyrazol-4-yl)carbonyl)-8-azabicyclo[3.2.1]octan-3-yl)amino)-6,7-difluoro-1-methylquinolin-2(1H)-one
-
4-(((1R,3R,5S)-8-((5-chloro-1-methyl-1H-pyrazol-4-yl)carbonyl)-8-azabicyclo[3.2.1]octan-3-yl)amino)-6-fluoro-1-methylquinolin-2(1H)-one
-
4-(((1R,3R,5S)-8-((5-chloro-1-methyl-1H-pyrazol-4-yl)carbonyl)-8-azabicyclo[3.2.1]octan-3-yl)amino)-6-fluoroquinolin-2(1H)-one
-
4-(((1R,3R,5S)-8-((5-chloro-1-methyl-1H-pyrazol-4-yl)carbonyl)-8-azabicyclo[3.2.1]octan-3-yl)amino)-6-phenylpyridin-2(1H)-one
-
4-(((1R,3S,5S)-8-((5-chloro-1-methyl-1H-pyrazol-4-yl)carbonyl)-8-azabicyclo[3.2.1]octan-3-yl)amino)-6-fluoroquinolin-2(1H)-one
-
4-(((2S,4R)-1-((5-chloro-1-methyl-1H-pyrazol-4-yl)carbonyl)-2-methylpiperidin-4-yl)amino)-6,7-difluoroquinolin-2(1H)-one
-
4-(((2S,4R)-1-((5-chloro-1-methyl-1H-pyrazol-4-yl)carbonyl)-2-methylpiperidin-4-yl)amino)quinolin-2(1H)-one
-
4-(((2S,4S)-1-((5-chloro-1-methyl-1H-pyrazol-4-yl)carbonyl)-2-methylpiperidin-4-yl)amino)quinolin-2(1H)-one
-
4-((1-((1,5-dimethyl-1H-1,2,3-triazol-4-yl)carbonyl)piperidin-4-yl)amino)-6-fluoroquinolin-2(1H)-one
-
4-((1-((1,5-dimethyl-1H-pyrazol-4-yl)carbonyl)piperidin-4-yl)-amino)quinolin-2(1H)-one
-
4-((1-((1-methyl-1H-pyrazol-4-yl)carbonyl)piperidin-4-yl)amino)-quinolin-2(1H)-one
-
4-((1-((4,5-dimethyl-1,2-oxazol-3-yl)carbonyl)piperidin-4-yl)-amino)-6,7-difluoroquinolin-2(1H)-one
-
4-((1-((4,5-dimethylisoxazol-3-yl)carbonyl)piperidin-4-yl)amino)-6,7-difluoro-1-methylquinolin-2(1H)-one
-
4-((1-((4,5-dimethylisoxazol-3-yl)carbonyl)piperidin-4-yl)amino)-6-fluoroquinolin-2(1H)-one
-
4-((1-((5-chloro-1-ethyl-1H-pyrazol-4-yl)carbonyl)piperidin-4-yl)-amino)-6-fluoroquinolin-2(1H)-one
-
4-((1-((5-chloro-1-isopropyl-1H-pyrazol-4-yl)carbonyl)piperidin-4-yl)amino)quinolin-2(1H)-one
-
4-((1-((5-chloro-1-methyl-1H-pyrazol-4-yl)carbonyl)azetidin-3-yl)amino)quinolin-2(1H)-one
-
4-((1-((5-chloro-1-methyl-1H-pyrazol-4-yl)carbonyl)piperidin-4-yl)amino)-1-ethylquinolin-2(1H)-one
-
4-((1-((5-chloro-1-methyl-1H-pyrazol-4-yl)carbonyl)piperidin-4-yl)amino)-1-methylquinolin-2(1H)-one
-
4-((1-((5-chloro-1-methyl-1H-pyrazol-4-yl)carbonyl)piperidin-4-yl)amino)-6,7-difluoro-1-methylquinolin-2(1H)-one
-
4-((1-((5-chloro-1-methyl-1H-pyrazol-4-yl)carbonyl)piperidin-4-yl)amino)-6,7-difluoroquinolin-2(1H)-one
-
4-((1-((5-chloro-1-methyl-1H-pyrazol-4-yl)carbonyl)piperidin-4-yl)amino)-6-fluoroquinolin-2(1H)-one
-
4-((1-((5-chloro-1-methyl-1H-pyrazol-4-yl)carbonyl)piperidin-4-yl)amino)-6-phenylpyridin-2(1H)-one
-
4-((1-((5-chloro-1-methyl-1H-pyrazol-4-yl)carbonyl)piperidin-4-yl)amino)-7,8-difluoroquinolin-2(1H)-one
-
4-((1-((5-chloro-1-methyl-1H-pyrazol-4-yl)carbonyl)piperidin-4-yl)amino)-7-fluoroquinolin-2(1H)-one
-
4-((1-((5-chloro-1-methyl-1H-pyrazol-4-yl)carbonyl)piperidin-4-yl)amino)-8-fluoroquinolin-2(1H)-one
-
4-((1-((5-chloro-1-methyl-1H-pyrazol-4-yl)carbonyl)piperidin-4-yl)amino)quinolin-2(1H)-one
-
4-((1-((5-chloro-1-methyl-1H-pyrazol-4-yl)carbonyl)piperidin-4-yl)methylamino)quinolin-2(1H)-one
-
4-((1-((5-chloro-1-methyl-1H-pyrazol-4-yl)carbonyl)piperidin-4-yl)oxy)quinolin-2(1H)-one
-
4-((1-((5-chloro-1-methyl-1H-pyrazol-4-yl)carbonyl)pyrrolidin-3-yl)amino)quinolin-2(1H)-one
-
4-((2-methoxyethyl)piperazin-1-yl)(7-nitro-5-(trifluoromethyl)benzo[d]thiazol-2-yl)methanone
-
4-((3-endo-8-((4,5-Dimethyl-1,2-oxazol-3-yl)carbonyl)-8-azabicyclo[3.2.1]oct-3-yl)amino)-6,7-difluoro-1-methylquinolin-2(1H)-one
-
4-((3-endo-8-((5-chloro-1-methyl-1H-pyrazol-4-yl)carbonyl)-8-azabicyclo[3.2.1]oct-3-yl)amino)-6,7-difluoroquinolin-2(1H)-one
-
4-((7-nitro-5-(trifluoromethyl)benzo[d]thiazol-2-yl)methyl)morpholine
-
4-benzyl-3-(3,5-dinitrophenyl)-5-[(4-methoxybenzyl)-sulfanyl]-4H-1,2,4-triazole
-
-
4-benzyl-3-(benzylsulfanyl)-5-(3,5-dinitrophenyl)-4H-1,2,4-triazole
-
-
4-benzyl-3-benzylsulfanyl-5-[3-nitro-5-(trifluoromethyl)-phenyl]-4H-1,2,4-triazole
-
-
4-benzyl-3-[(4-methoxybenzyl)sulfanyl]-5-[3-nitro-5-(trifluoromethyl)phenyl]-4H-1,2,4-triazole
-
-
5-((3,4-dimethylbenzylamino)methyl)-3-methyl-1-phenyl-1Hpyrazolo[3,4-b]pyridin-6(7H)-one
5-((3-fluorobenzylamino)methyl)-3-methyl-1-phenyl-1Hpyrazolo[3,4-b]pyridin-6(7H)-one
5-((benzylamino)methyl)-3-methyl-1-phenyl-1H-pyrazolo[3,4-b]-pyridin-6(7H)-one
6-bromo-3-methyl-8-nitro-2-phenylquinoline
-
-
6-fluoro-4-((1-((1-methyl-5-(trifluoromethyl)-1H-pyrazol-4-yl)-carbonyl)piperidin-4-yl)amino)quinolin-2(1H)-one
-
6-methyl-7-nitro-N-(pyridin-2-ylmethyl)-5-(trifluoromethyl)benzo[d]thiazole-2-carboxamide
-
7-nitro-2-(piperidine-1-carbonyl)-5-(trifluoromethyl)benzo[d]thiazole 3-oxide
-
7-nitro-2-(piperidine-1-carbonyl)benzo[d]thiazole-5-carbonitrile
-
7-nitro-2-(pyridin-2-ylmethylcarbamoyl)-5-(trifluoromethyl)benzo[d]thiazole 3-oxide
-
7-nitro-2-(pyridin-3-ylmethylcarbamoyl)-5-(trifluoromethyl)benzo[d]thiazole 3-oxide
-
7-nitro-5-((trifluoromethyl)-1,3-benzothiazol-2-yl)-piperidin-1-ylmethanone
-
7-nitro-N-(pyridin-2-ylmethyl)-5-(trifluoromethyl)benzo[d]thiazole-2-carboxamide
-
8-((3-endo-8-((4,5-dimethyl-1,2-oxazol-3-yl)carbonyl)-8-azabicyclo[3.2.1]oct-3-yl)amino)-5-methylpyrido[2,3-b]pyrazin-6(5H)-one
-
ethyl 1-[1-[5-(1H-pyrrol-1-yl)-1,3,4-thiadiazol-2-yl]piperidine-4-carbonyl]piperidine-4-carboxylate
-
ethyl {2-[(1,3-benzothiazole-2-carbonyl)amino]thiophene-3-carbonyl}carbamate
morpholino(7-nitro-5-(trifluoromethyl)benzo[d]thiazol-2-yl)methanone
-
N,N-dimethyl-1-[1-[5-(1H-pyrrol-1-yl)-1,3,4-thiadiazol-2-yl]piperidine-4-carbonyl]piperidine-4-carboxamide
-
N-(2-(4-methoxyphenoxy)ethyl)-3,5-dinitrobenzamide
more than a ten-fold decrease in the number of colony-forming units is observed with both human and mouse primary cells at a N-(2-(4-methoxyphenoxy) ethyl)-3,5-dinitrobenzamide concentrations above 5 microM, compound is also highly active against multidrug-resistant and extensively drug-resistant clinical isolates. N-(2-(4-methoxyphenoxy)ethyl)-3,5-dinitrobenzamide shows a clear-cut effect on the synthesis of the arabinan domains of arabinogalactan and lipoarabinomannan, and inhibition of decaprenyl-phospho-arabinose formation in the treated extracts concurrent with the accumulation of decaprenylphospho-ribose. Target of the inhibitors is probably the heteromeric decaprenylphospho-ribose 29 epimerase encoded by the dprE1/dprE2 genes
N-(2-(benzyloxy)ethyl)-3,5-dinitrobenzamide
more than a ten-fold decrease in the number of colony-forming units is observed with both human and mouse primary cells at a N-(2-(benzyloxy)ethyl)-3,5-dinitrobenzamide concentrations above 5 microM, compound is also highly active against multidrug-resistant and extensively drug-resistant clinical isolates. N-(2-(benzyloxy)ethyl)-3,5-dinitrobenzamide shows a clear-cut effect on the synthesis of the arabinan domains of arabinogalactan and lipoarabinomannan, and inhibition of decaprenyl-phospho-arabinose formation in the treated extracts concurrent with the accumulation of decaprenylphospho-ribose. Target of the inhibitors is probably the heteromeric decaprenylphospho-ribose 29 epimerase encoded by the dprE1/dprE2 genes
N-(2-fluoroethyl)-1-((6-methoxy-5-methylpyrimidin-4-yl)methyl)-1H-pyrrolo[3,2-b]pyridine-3-carboxamide
-
N-(2-fluoroethyl)-1-[(6-methoxy-5-methylpyrimidin-4-yl)methyl]-1H-pyrrolo[3,2-b]pyridine-3-carboxamide
N-(pyridin-2-ylmethyl)-5-(trifluoromethyl)benzo[d]thiazole-2-carboxamide
-
N-methyl-7-nitro-2-(piperidine-1-carbonyl)benzo[d]thiazole-5-carboxamide
-
N-[(2S)-3-hydroxy-1-oxo-1-pyrrolidin-1-ylpropan-2-yl]-7-nitro-5-(trifluoromethyl)-1,3-benzothiazole-2-carboxamide
-
N-[2-(4-methoxyphenoxy)ethyl]-3,5-dinitrobenzamide
-
-
[4-[(2H-1,3-benzodioxol-5-yl)methyl]piperazin-1-yl][1-[5-(1H-pyrrol-1-yl)-1,3,4-thiadiazol-2-yl]piperidin-4-yl]methanone
-
[4-[(4-fluorophenyl)methyl]piperidin-1-yl][1-[5-(1H-pyrrol-1-yl)-1,3,4-thiadiazol-2-yl]piperidin-4-yl]methanone
-
[4-[(methylamino)methyl]piperidin-1-yl][1-[5-(1H-pyrrol-1-yl)-1,3,4-thiadiazol-2-yl]piperidin-4-yl]methanone
-
[4-[(pyridin-2-yl)methyl]piperidin-1-yl][1-[5-(1H-pyrrol-1-yl)-1,3,4-thiadiazol-2-yl]piperidin-4-yl]methanone
-
[4-[(pyridin-3-yl)methyl]piperidin-1-yl][1-[5-(1H-pyrrol-1-yl)-1,3,4-thiadiazol-2-yl]piperidin-4-yl]methanone
-
1,3-dimethyl-5-((3-(trifluoromethyl)benzylamino)methyl)-1Hpyrazolo[3,4-b]pyridin-6(7H)-one
-
1,3-dimethyl-5-((3-(trifluoromethyl)benzylamino)methyl)-1Hpyrazolo[3,4-b]pyridin-6(7H)-one
-
1-(6-methoxy-3-methyl-1-phenyl-1H-pyrazolo[3,4-b]pyridin-5-yl)-N-(3-(trifluoromethyl)benzyl)methanamine
-
1-(6-methoxy-3-methyl-1-phenyl-1H-pyrazolo[3,4-b]pyridin-5-yl)-N-(3-(trifluoromethyl)benzyl)methanamine
-
2-[(2S)-2-methyl-1,4-dioxa-8-azaspiro[4.5]dec-8-yl]-8-nitro-6-(trifluoromethyl)-4H-1,3-benzothiazin-4-one
tuberculosis drug candidate with high activity against Mycobacterium tuberculosis in vitro and in vivo. Compound is activated in the bacterium by reduction of an essential nitro group to a nitroso derivative, which then specifically reacts with a cysteine residue in the active site of DprE1
2-[(2S)-2-methyl-1,4-dioxa-8-azaspiro[4.5]dec-8-yl]-8-nitro-6-(trifluoromethyl)-4H-1,3-benzothiazin-4-one
i.e. BTZ043, inhibits enzyme by formation of a semimercaptal
2-[(2S)-2-methyl-1,4-dioxa-8-azaspiro[4.5]decan-8-yl]-8-nitro-6-(trifluoromethyl)-4H-1,3-benzothiazin-4-one
-
-
2-[(2S)-2-methyl-1,4-dioxa-8-azaspiro[4.5]decan-8-yl]-8-nitro-6-(trifluoromethyl)-4H-1,3-benzothiazin-4-one
BTZ043
2-[(2S)-2-methyl-1,4-dioxa-8-azaspiro[4.5]decan-8-yl]-8-nitro-6-(trifluoromethyl)-4H-1,3-benzothiazin-4-one
BTZ043
2-[4-(cyclohexylmethyl)piperazin-1-yl]-8-nitro-6-(trifluoromethyl)-4H-1,3-benzothiazin-4-one
PBTZ169
2-[4-(cyclohexylmethyl)piperazin-1-yl]-8-nitro-6-(trifluoromethyl)-4H-1,3-benzothiazin-4-one
complete inhibition at 0.04 mM
2-[4-(cyclohexylmethyl)piperazin-1-yl]-8-nitro-6-(trifluoromethyl)-4H-1,3-benzothiazin-4-one
PBTZ169
2-[4-(cyclohexylmethyl)piperazin-1-yl]-8-nitro-6-(trifluoromethyl)-4H-1,3-benzothiazin-4-one
PBTZ169
3,7-dimethyl-1-phenyl-5-((3-(trifluoromethyl)benzylamino)-methyl)-1H-pyrazolo[3,4-b]pyridin-6(7H)-one
-
3,7-dimethyl-1-phenyl-5-((3-(trifluoromethyl)benzylamino)-methyl)-1H-pyrazolo[3,4-b]pyridin-6(7H)-one
-
3-(((3-methyl-6-oxo-1-phenyl-6,7-dihydro-1H-pyrazolo[3,4-b]-pyridin-5-yl)methylamino)methyl)benzonitrile
-
3-(((3-methyl-6-oxo-1-phenyl-6,7-dihydro-1H-pyrazolo[3,4-b]-pyridin-5-yl)methylamino)methyl)benzonitrile
-
3-cyclopropyl-1-phenyl-5-(((6-(trifluoromethyl)pyridin-2-yl)-methylamino)methyl)-1H-pyrazolo[3,4-b]pyridin-6(7H)-one
-
3-cyclopropyl-1-phenyl-5-(((6-(trifluoromethyl)pyridin-2-yl)-methylamino)methyl)-1H-pyrazolo[3,4-b]pyridin-6(7H)-one
-
3-cyclopropyl-1-phenyl-5-((3-(trifluoromethyl)benzylamino)-methyl)-1H-pyrazolo[3,4-b]pyridin-6(7H)-one
-
3-cyclopropyl-1-phenyl-5-((3-(trifluoromethyl)benzylamino)-methyl)-1H-pyrazolo[3,4-b]pyridin-6(7H)-one
-
3-cyclopropyl-5-(((3-methyl-6-(trifluoromethyl)pyridin-2-yl)-methylamino)methyl)-1-phenyl-1H-pyrazolo[3,4-b]pyridin-6(7H)-one
-
3-cyclopropyl-5-(((3-methyl-6-(trifluoromethyl)pyridin-2-yl)-methylamino)methyl)-1-phenyl-1H-pyrazolo[3,4-b]pyridin-6(7H)-one
-
3-cyclopropyl-5-((2-fluoro-3-(trifluoromethyl)benzylamino)-methyl)-1-phenyl-1H-pyrazolo[3,4-b]pyridin-6(7H)-one
-
3-cyclopropyl-5-((2-fluoro-3-(trifluoromethyl)benzylamino)-methyl)-1-phenyl-1H-pyrazolo[3,4-b]pyridin-6(7H)-one
-
3-cyclopropyl-5-((2-fluoro-5-(trifluoromethyl)benzylamino)-methyl)-1-phenyl-1H-pyrazolo[3,4-b]pyridin-6(7H)-one
-
3-cyclopropyl-5-((2-fluoro-5-(trifluoromethyl)benzylamino)-methyl)-1-phenyl-1H-pyrazolo[3,4-b]pyridin-6(7H)-one
-
3-cyclopropyl-5-((2-methyl-5-(trifluoromethyl)benzylamino)-methyl)-1-phenyl-1H-pyrazolo[3,4-b]pyridin-6(7H)-one
-
3-cyclopropyl-5-((2-methyl-5-(trifluoromethyl)benzylamino)-methyl)-1-phenyl-1H-pyrazolo[3,4-b]pyridin-6(7H)-one
-
3-isopropyl-5-((2-methyl-5-(trifluoromethyl)benzylamino)-methyl)-1-phenyl-1H-pyrazolo[3,4-b]pyridin-6(7H)-one
-
3-isopropyl-5-((2-methyl-5-(trifluoromethyl)benzylamino)-methyl)-1-phenyl-1H-pyrazolo[3,4-b]pyridin-6(7H)-one
-
3-methyl-1-(pyridin-2-yl)-5-((3-(trifluoromethyl)benzylamino)-methyl)-1H-pyrazolo[3,4-b]pyridin-6(7H)-one
-
3-methyl-1-(pyridin-2-yl)-5-((3-(trifluoromethyl)benzylamino)-methyl)-1H-pyrazolo[3,4-b]pyridin-6(7H)-one
-
3-methyl-1-p-tolyl-5-((3-(trifluoromethyl)benzylamino)methyl)-1H-pyrazolo[3,4-b]pyridin-6(7H)-one
-
3-methyl-1-p-tolyl-5-((3-(trifluoromethyl)benzylamino)methyl)-1H-pyrazolo[3,4-b]pyridin-6(7H)-one
-
3-methyl-1-phenyl-5-((3-(trifluoromethyl)benzylamino)methyl)-1H-pyrazolo[3,4-b]pyridin-6(7H)-one
-
3-methyl-1-phenyl-5-((3-(trifluoromethyl)benzylamino)methyl)-1H-pyrazolo[3,4-b]pyridin-6(7H)-one
-
3-methyl-1-phenyl-5-((7-(trifluoromethyl)-3,4-dihydroisoquinolin-2(1H)-yl)methyl)-1H-pyrazolo[3,4-b]pyridin-6(7H)-one
-
3-methyl-1-phenyl-5-((7-(trifluoromethyl)-3,4-dihydroisoquinolin-2(1H)-yl)methyl)-1H-pyrazolo[3,4-b]pyridin-6(7H)-one
-
3-methyl-5-((2-methyl-5-(trifluoromethyl)benzylamino)methyl)-1-phenyl-1H-pyrazolo[3,4-b]pyridin-6(7H)-one
-
3-methyl-5-((2-methyl-5-(trifluoromethyl)benzylamino)methyl)-1-phenyl-1H-pyrazolo[3,4-b]pyridin-6(7H)-one
-
3-methyl-5-((3-methylbenzylamino)methyl)-1-phenyl-1Hpyrazolo[3,4-b]pyridin-6(7H)-one
-
3-methyl-5-((3-methylbenzylamino)methyl)-1-phenyl-1Hpyrazolo[3,4-b]pyridin-6(7H)-one
-
3-methyl-5-((methyl(3-(trifluoromethyl)benzyl)amino)methyl)-1-phenyl-1H-pyrazolo[3,4-b]pyridin-6(7H)-one
-
3-methyl-5-((methyl(3-(trifluoromethyl)benzyl)amino)methyl)-1-phenyl-1H-pyrazolo[3,4-b]pyridin-6(7H)-one
-
3-methyl-6-oxo-1-phenyl-N-(3-(trifluoromethyl)benzyl)-6,7-dihydro-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
-
3-methyl-6-oxo-1-phenyl-N-(3-(trifluoromethyl)benzyl)-6,7-dihydro-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
-
3-nitro-N-[(1R)-1-phenylethyl]-5-(trifluoromethyl)benzamide
high activity against Mycobacterium smegmatis and Mycobacterium tuberculosis H37Rv but no significant activity against benzothiazinone-resistant strains with the mutations Cys387Ser or Cys387Gly in DprE1
3-nitro-N-[(1R)-1-phenylethyl]-5-(trifluoromethyl)benzamide
forms a noncovalent complex with the enzyme
3-nitro-N-[(1R)-1-phenylethyl]-5-(trifluoromethyl)benzamide
-
-
5-((3,4-dimethylbenzylamino)methyl)-3-methyl-1-phenyl-1Hpyrazolo[3,4-b]pyridin-6(7H)-one
-
5-((3,4-dimethylbenzylamino)methyl)-3-methyl-1-phenyl-1Hpyrazolo[3,4-b]pyridin-6(7H)-one
-
5-((3-fluorobenzylamino)methyl)-3-methyl-1-phenyl-1Hpyrazolo[3,4-b]pyridin-6(7H)-one
-
5-((3-fluorobenzylamino)methyl)-3-methyl-1-phenyl-1Hpyrazolo[3,4-b]pyridin-6(7H)-one
-
5-((benzylamino)methyl)-3-methyl-1-phenyl-1H-pyrazolo[3,4-b]-pyridin-6(7H)-one
-
5-((benzylamino)methyl)-3-methyl-1-phenyl-1H-pyrazolo[3,4-b]-pyridin-6(7H)-one
-
BTZ043
-
ethyl {2-[(1,3-benzothiazole-2-carbonyl)amino]thiophene-3-carbonyl}carbamate
-
-
ethyl {2-[(1,3-benzothiazole-2-carbonyl)amino]thiophene-3-carbonyl}carbamate
TCA1
ethyl {2-[(1,3-benzothiazole-2-carbonyl)amino]thiophene-3-carbonyl}carbamate
TCA1
N-(2-fluoroethyl)-1-[(6-methoxy-5-methylpyrimidin-4-yl)methyl]-1H-pyrrolo[3,2-b]pyridine-3-carboxamide
-
N-(2-fluoroethyl)-1-[(6-methoxy-5-methylpyrimidin-4-yl)methyl]-1H-pyrrolo[3,2-b]pyridine-3-carboxamide
-
PBTZ169
-
additional information
not inhibited by rifampin
-
additional information
-
not inhibited by rifampin
-
additional information
benzothiazinone and dinitrobenzamide inhibitors target decaprenylphospho-beta-D-ribofuranose 2-oxidase DprE1. Several mutants showing high levels of dinitrobenzamide resistance, exhibit a mutation in residue Cys394 of DprE1
-
additional information
-
benzothiazinone and dinitrobenzamide inhibitors target decaprenylphospho-beta-D-ribofuranose 2-oxidase DprE1. Several mutants showing high levels of dinitrobenzamide resistance, exhibit a mutation in residue Cys394 of DprE1
-
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0.00026
(3,4-dihydroisoquinolin-2(1H)-yl)[1-[5-(1H-pyrrol-1-yl)-1,3,4-thiadiazol-2-yl]piperidin-4-yl]methanone
Mycobacterium tuberculosis
at pH 7.5 and 22°C
0.0017
(4-(2-methoxyethyl)piperazin-1-yl)(6-methyl-7-nitro-5-(trifluoromethyl)benzo[d]thiazol-2-yl)methanone
Mycobacterium tuberculosis
pH and temperature not specified in the publication
0.0012
(4-benzylpiperazin-1-yl)[1-[5-(1H-pyrrol-1-yl)-1,3,4-thiadiazol-2-yl]piperidin-4-yl]methanone
Mycobacterium tuberculosis
at pH 7.5 and 22°C
0.0017
(4-methylpiperidin-1-yl)[1-[5-(1H-pyrrol-1-yl)-1,3,4-thiadiazol-2-yl]piperidin-4-yl]methanone
Mycobacterium tuberculosis
at pH 7.5 and 22°C
0.00012
(5-chloro-1-methyl-1H-pyrazol-4-yl)(3-endo-3-((5-fluoro-1H-indazol-3-yl)amino)-8-azabicyclo[3.2.1]oct-8-yl)methanone
Mycobacterium tuberculosis
at pH 8.5 and 25°C
0.078
(5-chloro-1-methyl-1H-pyrazol-4-yl)(4-((2-methoxyquinolin-4-yl)amino)piperidin-1-yl)methanone
Mycobacterium tuberculosis
at pH 8.5 and 25°C
0.00013
(5-chloro-1-methyl-1H-pyrazol-4-yl)(4-((5-fluoro-1H-indazol-3-yl)amino)piperidin-1-yl)methanone
Mycobacterium tuberculosis
at pH 8.5 and 25°C
0.01
(5-chloro-1-methyl-1H-pyrazol-4-yl)(4-(cinnolin-4-ylamino)-piperidin-1-yl)methanone
Mycobacterium tuberculosis
IC50 above 0.01 mM, at pH 8.5 and 25°C
0.0022
(6-methyl-7-nitro-5-(trifluoromethyl)benzo[d]thiazol-2-yl)(piperidin-1-yl)methanone
Mycobacterium tuberculosis
pH and temperature not specified in the publication
0.0012
(S)-(2-(6-methyl-7-nitro-5-(trifluoromethyl)benzo[d]thiazol-2-yl)-4,5-dihydrooxazol-4-yl)(pyrrolidin-1-yl)methanone
Mycobacterium tuberculosis
pH and temperature not specified in the publication
0.000654
(S)-(2-(7-nitro-5-(trifluoromethyl)benzo[d]thiazol-2-yl)-4,5-dihydrooxazol-4-yl)(pyrrolidin-1-yl)methanone
Mycobacterium tuberculosis
pH and temperature not specified in the publication
0.00006
(S)-7-nitro-2-(1-oxo-1-(pyrrolidin-1-yl)propan-2-ylcarbamoyl)-5-(trifluoromethyl)benzo[d]thiazole 3-oxide
Mycobacterium tuberculosis
pH and temperature not specified in the publication
0.0012
(S)-N-(3-hydroxy-1-oxo-1-(pyrrolidin-1-yl)propan-2-yl)-6-methyl-7-nitro-5-(trifluoromethyl)benzo[d]thiazole-2-carboxamide
Mycobacterium tuberculosis
pH and temperature not specified in the publication
0.0012
(S)-N-(4-hydroxy-1-oxo-1-(piperidin-1-yl)butan-2-yl)-6-methyl-7-nitro-5-(trifluoromethyl)benzo[d]thiazole-2-carboxamide
Mycobacterium tuberculosis
pH and temperature not specified in the publication
0.1
1,3-dimethyl-5-((3-(trifluoromethyl)benzylamino)methyl)-1Hpyrazolo[3,4-b]pyridin-6(7H)-one
Mycolicibacterium smegmatis
IC50 above 0.1 mM, pH and temperature not specified in the publication
0.01
1-(6-methoxy-3-methyl-1-phenyl-1H-pyrazolo[3,4-b]pyridin-5-yl)-N-(3-(trifluoromethyl)benzyl)methanamine
Mycolicibacterium smegmatis
IC50 above 0.01 mM, pH and temperature not specified in the publication
0.1
1-[1-[5-(1H-pyrrol-1-yl)-1,3,4-thiadiazol-2-yl]piperidine-4-carbonyl]piperidine-4-carboxylic acid
Mycobacterium tuberculosis
IC50 above 0.1 mM, at pH 7.5 and 22°C
0.000276
2-(4,5-dihydrooxazol-2-yl)-7-nitro-5-(trifluoromethyl)benzo[d]thiazole 3-oxide
Mycobacterium tuberculosis
pH and temperature not specified in the publication
0.000027
2-(4-(2-methoxyethyl)piperazine-1-carbonyl)-7-nitro-5-(trifluoromethyl)benzo[d]thiazole 3-oxide
Mycobacterium tuberculosis
pH and temperature not specified in the publication
0.0039
2-(6-methyl-7-nitro-5-(trifluoromethyl)benzo[d]thiazol-2-yl)-4,5-dihydrooxazole
Mycobacterium tuberculosis
pH and temperature not specified in the publication
0.0059
2-(methoxymethyl)-7-nitro-5-(trifluoromethyl)benzo[d]thiazole
Mycobacterium tuberculosis
pH and temperature not specified in the publication
0.1
2-(piperidine-1-carbonyl)-5-(trifluoromethyl)benzo[d]thiazole-7-carboxylic acid
Mycobacterium tuberculosis
IC50 above 0.1 mM, pH and temperature not specified in the publication
0.00161
2-[(2S)-2-methyl-1,4-dioxa-8-azaspiro[4,5]dec-8-yl]-8-(1H-pyrrol-1-yl)-6-(trifluoromethyl)-4H-1,3-benzothiazin-4-one
Mycobacterium tuberculosis
at pH 7.5 and 30°C
0.00000425
2-[(2S)-2-methyl-1,4-dioxa-8-azaspiro[4,5]dec-8-yl]-8-nitro-6-(trifluoromethyl)-4H-1,3-benzothiazin-4-one
Mycobacterium tuberculosis
at pH 7.5 and 30°C
0.00734
2-[4-(cyclohexylmethyl)piperazin-1-yl]-8-(1H-pyrrol-1-yl)-6-(trifluoromethyl)-4H-1,3-benzothiazin-4-one
Mycobacterium tuberculosis
at pH 7.5 and 30°C
0.01
3,7-dimethyl-1-phenyl-5-((3-(trifluoromethyl)benzylamino)-methyl)-1H-pyrazolo[3,4-b]pyridin-6(7H)-one
Mycolicibacterium smegmatis
IC50 above 0.01 mM, pH and temperature not specified in the publication
0.0026
3-(((3-methyl-6-oxo-1-phenyl-6,7-dihydro-1H-pyrazolo[3,4-b]-pyridin-5-yl)methylamino)methyl)benzonitrile
Mycolicibacterium smegmatis
pH and temperature not specified in the publication
0.0282
3-(2-(piperidine-1-carbonyl)-5-(trifluoromethyl)benzo[d]thiazol-7-yl)-1,2,3-oxadiazol-3-ium-5-olate
Mycobacterium tuberculosis
pH and temperature not specified in the publication
0.0005
3-cyclopropyl-1-phenyl-5-(((6-(trifluoromethyl)pyridin-2-yl)-methylamino)methyl)-1H-pyrazolo[3,4-b]pyridin-6(7H)-one
Mycolicibacterium smegmatis
pH and temperature not specified in the publication
0.00004
3-cyclopropyl-1-phenyl-5-((3-(trifluoromethyl)benzylamino)-methyl)-1H-pyrazolo[3,4-b]pyridin-6(7H)-one
Mycolicibacterium smegmatis
pH and temperature not specified in the publication
0.00001
3-cyclopropyl-5-(((3-methyl-6-(trifluoromethyl)pyridin-2-yl)-methylamino)methyl)-1-phenyl-1H-pyrazolo[3,4-b]pyridin-6(7H)-one
Mycolicibacterium smegmatis
pH and temperature not specified in the publication
0.000005
3-cyclopropyl-5-((2-fluoro-3-(trifluoromethyl)benzylamino)-methyl)-1-phenyl-1H-pyrazolo[3,4-b]pyridin-6(7H)-one
Mycolicibacterium smegmatis
pH and temperature not specified in the publication
0.00007
3-cyclopropyl-5-((2-fluoro-5-(trifluoromethyl)benzylamino)-methyl)-1-phenyl-1H-pyrazolo[3,4-b]pyridin-6(7H)-one
Mycolicibacterium smegmatis
pH and temperature not specified in the publication
0.00001
3-cyclopropyl-5-((2-methyl-5-(trifluoromethyl)benzylamino)-methyl)-1-phenyl-1H-pyrazolo[3,4-b]pyridin-6(7H)-one
Mycolicibacterium smegmatis
pH and temperature not specified in the publication
0.000005
3-isopropyl-5-((2-methyl-5-(trifluoromethyl)benzylamino)-methyl)-1-phenyl-1H-pyrazolo[3,4-b]pyridin-6(7H)-one
Mycolicibacterium smegmatis
pH and temperature not specified in the publication
0.0006
3-methyl-1-p-tolyl-5-((3-(trifluoromethyl)benzylamino)methyl)-1H-pyrazolo[3,4-b]pyridin-6(7H)-one
Mycolicibacterium smegmatis
pH and temperature not specified in the publication
0.0004
3-methyl-1-phenyl-5-((3-(trifluoromethyl)benzylamino)methyl)-1H-pyrazolo[3,4-b]pyridin-6(7H)-one
Mycolicibacterium smegmatis
pH and temperature not specified in the publication
0.0062
3-methyl-1-phenyl-5-((7-(trifluoromethyl)-3,4-dihydroisoquinolin-2(1H)-yl)methyl)-1H-pyrazolo[3,4-b]pyridin-6(7H)-one
Mycolicibacterium smegmatis
pH and temperature not specified in the publication
0.000007
3-methyl-5-((2-methyl-5-(trifluoromethyl)benzylamino)methyl)-1-phenyl-1H-pyrazolo[3,4-b]pyridin-6(7H)-one
Mycolicibacterium smegmatis
pH and temperature not specified in the publication
0.0028
3-methyl-5-((3-methylbenzylamino)methyl)-1-phenyl-1Hpyrazolo[3,4-b]pyridin-6(7H)-one
Mycolicibacterium smegmatis
pH and temperature not specified in the publication
0.00006
3-methyl-5-((methyl(3-(trifluoromethyl)benzyl)amino)methyl)-1-phenyl-1H-pyrazolo[3,4-b]pyridin-6(7H)-one
Mycolicibacterium smegmatis
pH and temperature not specified in the publication
0.001
3-methyl-6-oxo-1-phenyl-N-(3-(trifluoromethyl)benzyl)-6,7-dihydro-1H-pyrazolo[3,4-b]pyridine-5-carboxamide
Mycolicibacterium smegmatis
pH and temperature not specified in the publication
0.000007
4-(((1R,3R,5S)-8-((4,5-dimethylisoxazol-3-yl)carbonyl)-8-azabicyclo[3.2.1]octan-3-yl)amino)-6,7-difluoroquinolin-2(1H)-one
Mycobacterium tuberculosis
at pH 8.5 and 25°C
0.000026
4-(((1R,3R,5S)-8-((5-chloro-1-methyl-1H-pyrazol-4-yl)carbonyl)-8-azabicyclo[3.2.1]octan-3-yl)amino)-1-methyl-1,8-naphthyridin-2(1H)-one
Mycobacterium tuberculosis
at pH 8.5 and 25°C
0.000008
4-(((1R,3R,5S)-8-((5-chloro-1-methyl-1H-pyrazol-4-yl)carbonyl)-8-azabicyclo[3.2.1]octan-3-yl)amino)-6,7-difluoro-1-methylquinolin-2(1H)-one
Mycobacterium tuberculosis
at pH 8.5 and 25°C
0.000012
4-(((1R,3R,5S)-8-((5-chloro-1-methyl-1H-pyrazol-4-yl)carbonyl)-8-azabicyclo[3.2.1]octan-3-yl)amino)-6-fluoro-1-methylquinolin-2(1H)-one
Mycobacterium tuberculosis
at pH 8.5 and 25°C
0.00003
4-(((1R,3R,5S)-8-((5-chloro-1-methyl-1H-pyrazol-4-yl)carbonyl)-8-azabicyclo[3.2.1]octan-3-yl)amino)-6-fluoroquinolin-2(1H)-one
Mycobacterium tuberculosis
at pH 8.5 and 25°C
0.000053
4-(((1R,3R,5S)-8-((5-chloro-1-methyl-1H-pyrazol-4-yl)carbonyl)-8-azabicyclo[3.2.1]octan-3-yl)amino)-6-phenylpyridin-2(1H)-one
Mycobacterium tuberculosis
at pH 8.5 and 25°C
0.043
4-(((1R,3S,5S)-8-((5-chloro-1-methyl-1H-pyrazol-4-yl)carbonyl)-8-azabicyclo[3.2.1]octan-3-yl)amino)-6-fluoroquinolin-2(1H)-one
Mycobacterium tuberculosis
at pH 8.5 and 25°C
0.000021
4-(((2S,4R)-1-((5-chloro-1-methyl-1H-pyrazol-4-yl)carbonyl)-2-methylpiperidin-4-yl)amino)-6,7-difluoroquinolin-2(1H)-one
Mycobacterium tuberculosis
at pH 8.5 and 25°C
0.000026
4-(((2S,4R)-1-((5-chloro-1-methyl-1H-pyrazol-4-yl)carbonyl)-2-methylpiperidin-4-yl)amino)quinolin-2(1H)-one
Mycobacterium tuberculosis
at pH 8.5 and 25°C
0.01
4-(((2S,4S)-1-((5-chloro-1-methyl-1H-pyrazol-4-yl)carbonyl)-2-methylpiperidin-4-yl)amino)quinolin-2(1H)-one
Mycobacterium tuberculosis
IC50 above 0.01 mM, at pH 8.5 and 25°C
0.000011
4-((1-((1,5-dimethyl-1H-1,2,3-triazol-4-yl)carbonyl)piperidin-4-yl)amino)-6-fluoroquinolin-2(1H)-one
Mycobacterium tuberculosis
at pH 8.5 and 25°C
0.00021
4-((1-((1,5-dimethyl-1H-pyrazol-4-yl)carbonyl)piperidin-4-yl)-amino)quinolin-2(1H)-one
Mycobacterium tuberculosis
at pH 8.5 and 25°C
0.0022
4-((1-((1-methyl-1H-pyrazol-4-yl)carbonyl)piperidin-4-yl)amino)-quinolin-2(1H)-one
Mycobacterium tuberculosis
at pH 8.5 and 25°C
0.000018
4-((1-((4,5-dimethyl-1,2-oxazol-3-yl)carbonyl)piperidin-4-yl)-amino)-6,7-difluoroquinolin-2(1H)-one
Mycobacterium tuberculosis
at pH 8.5 and 25°C
0.000038
4-((1-((4,5-dimethylisoxazol-3-yl)carbonyl)piperidin-4-yl)amino)-6,7-difluoro-1-methylquinolin-2(1H)-one
Mycobacterium tuberculosis
at pH 8.5 and 25°C
0.000006
4-((1-((4,5-dimethylisoxazol-3-yl)carbonyl)piperidin-4-yl)amino)-6-fluoroquinolin-2(1H)-one
Mycobacterium tuberculosis
at pH 8.5 and 25°C
0.000045
4-((1-((5-chloro-1-ethyl-1H-pyrazol-4-yl)carbonyl)piperidin-4-yl)-amino)-6-fluoroquinolin-2(1H)-one
Mycobacterium tuberculosis
at pH 8.5 and 25°C
0.007
4-((1-((5-chloro-1-isopropyl-1H-pyrazol-4-yl)carbonyl)piperidin-4-yl)amino)quinolin-2(1H)-one
Mycobacterium tuberculosis
at pH 8.5 and 25°C
0.0018
4-((1-((5-chloro-1-methyl-1H-pyrazol-4-yl)carbonyl)azetidin-3-yl)amino)quinolin-2(1H)-one
Mycobacterium tuberculosis
at pH 8.5 and 25°C
0.1
4-((1-((5-chloro-1-methyl-1H-pyrazol-4-yl)carbonyl)piperidin-4-yl)amino)-1-ethylquinolin-2(1H)-one
Mycobacterium tuberculosis
IC50 above 0.1 mM, at pH 8.5 and 25°C
0.00014
4-((1-((5-chloro-1-methyl-1H-pyrazol-4-yl)carbonyl)piperidin-4-yl)amino)-1-methylquinolin-2(1H)-one
Mycobacterium tuberculosis
at pH 8.5 and 25°C
0.00002
4-((1-((5-chloro-1-methyl-1H-pyrazol-4-yl)carbonyl)piperidin-4-yl)amino)-6,7-difluoro-1-methylquinolin-2(1H)-one
Mycobacterium tuberculosis
at pH 8.5 and 25°C
0.000006
4-((1-((5-chloro-1-methyl-1H-pyrazol-4-yl)carbonyl)piperidin-4-yl)amino)-6,7-difluoroquinolin-2(1H)-one
Mycobacterium tuberculosis
at pH 8.5 and 25°C
0.000005
4-((1-((5-chloro-1-methyl-1H-pyrazol-4-yl)carbonyl)piperidin-4-yl)amino)-6-fluoroquinolin-2(1H)-one
Mycobacterium tuberculosis
at pH 8.5 and 25°C
0.003
4-((1-((5-chloro-1-methyl-1H-pyrazol-4-yl)carbonyl)piperidin-4-yl)amino)-6-phenylpyridin-2(1H)-one
Mycobacterium tuberculosis
at pH 8.5 and 25°C
0.000009
4-((1-((5-chloro-1-methyl-1H-pyrazol-4-yl)carbonyl)piperidin-4-yl)amino)-7,8-difluoroquinolin-2(1H)-one
Mycobacterium tuberculosis
at pH 8.5 and 25°C
0.000007
4-((1-((5-chloro-1-methyl-1H-pyrazol-4-yl)carbonyl)piperidin-4-yl)amino)-7-fluoroquinolin-2(1H)-one
Mycobacterium tuberculosis
at pH 8.5 and 25°C
0.000011
4-((1-((5-chloro-1-methyl-1H-pyrazol-4-yl)carbonyl)piperidin-4-yl)amino)-8-fluoroquinolin-2(1H)-one
Mycobacterium tuberculosis
at pH 8.5 and 25°C
0.018
4-((1-((5-chloro-1-methyl-1H-pyrazol-4-yl)carbonyl)piperidin-4-yl)methylamino)quinolin-2(1H)-one
Mycobacterium tuberculosis
at pH 8.5 and 25°C
0.008
4-((1-((5-chloro-1-methyl-1H-pyrazol-4-yl)carbonyl)piperidin-4-yl)oxy)quinolin-2(1H)-one
Mycobacterium tuberculosis
at pH 8.5 and 25°C
0.0047
4-((1-((5-chloro-1-methyl-1H-pyrazol-4-yl)carbonyl)pyrrolidin-3-yl)amino)quinolin-2(1H)-one
Mycobacterium tuberculosis
at pH 8.5 and 25°C
0.000247
4-((2-methoxyethyl)piperazin-1-yl)(7-nitro-5-(trifluoromethyl)benzo[d]thiazol-2-yl)methanone
Mycobacterium tuberculosis
pH and temperature not specified in the publication
0.000017
4-((3-endo-8-((4,5-Dimethyl-1,2-oxazol-3-yl)carbonyl)-8-azabicyclo[3.2.1]oct-3-yl)amino)-6,7-difluoro-1-methylquinolin-2(1H)-one
Mycobacterium tuberculosis
at pH 8.5 and 25°C
0.000009
4-((3-endo-8-((5-chloro-1-methyl-1H-pyrazol-4-yl)carbonyl)-8-azabicyclo[3.2.1]oct-3-yl)amino)-6,7-difluoroquinolin-2(1H)-one
Mycobacterium tuberculosis
at pH 8.5 and 25°C
0.0052
4-((7-nitro-5-(trifluoromethyl)benzo[d]thiazol-2-yl)methyl)morpholine
Mycobacterium tuberculosis
pH and temperature not specified in the publication
0.0012
5-((3,4-dimethylbenzylamino)methyl)-3-methyl-1-phenyl-1Hpyrazolo[3,4-b]pyridin-6(7H)-one
Mycolicibacterium smegmatis
pH and temperature not specified in the publication
0.002
5-((3-fluorobenzylamino)methyl)-3-methyl-1-phenyl-1Hpyrazolo[3,4-b]pyridin-6(7H)-one
Mycolicibacterium smegmatis
pH and temperature not specified in the publication
0.0014
5-((benzylamino)methyl)-3-methyl-1-phenyl-1H-pyrazolo[3,4-b]-pyridin-6(7H)-one
Mycolicibacterium smegmatis
pH and temperature not specified in the publication
0.000021
6-fluoro-4-((1-((1-methyl-5-(trifluoromethyl)-1H-pyrazol-4-yl)-carbonyl)piperidin-4-yl)amino)quinolin-2(1H)-one
Mycobacterium tuberculosis
at pH 8.5 and 25°C
0.0012
6-methyl-7-nitro-N-(pyridin-2-ylmethyl)-5-(trifluoromethyl)benzo[d]thiazole-2-carboxamide
Mycobacterium tuberculosis
pH and temperature not specified in the publication
0.000095
7-nitro-2-(piperidine-1-carbonyl)-5-(trifluoromethyl)benzo[d]thiazole 3-oxide
Mycobacterium tuberculosis
pH and temperature not specified in the publication
0.0018
7-nitro-2-(piperidine-1-carbonyl)benzo[d]thiazole-5-carbonitrile
Mycobacterium tuberculosis
pH and temperature not specified in the publication
0.000026
7-nitro-2-(pyridin-2-ylmethylcarbamoyl)-5-(trifluoromethyl)benzo[d]thiazole 3-oxide
Mycobacterium tuberculosis
pH and temperature not specified in the publication
0.000213
7-nitro-5-((trifluoromethyl)-1,3-benzothiazol-2-yl)-piperidin-1-ylmethanone
Mycobacterium tuberculosis
pH and temperature not specified in the publication
0.000452
7-nitro-N-(pyridin-2-ylmethyl)-5-(trifluoromethyl)benzo[d]thiazole-2-carboxamide
Mycobacterium tuberculosis
pH and temperature not specified in the publication
0.000183
8-((3-endo-8-((4,5-dimethyl-1,2-oxazol-3-yl)carbonyl)-8-azabicyclo[3.2.1]oct-3-yl)amino)-5-methylpyrido[2,3-b]pyrazin-6(5H)-one
Mycobacterium tuberculosis
at pH 8.5 and 25°C
0.0036
ethyl 1-[1-[5-(1H-pyrrol-1-yl)-1,3,4-thiadiazol-2-yl]piperidine-4-carbonyl]piperidine-4-carboxylate
Mycobacterium tuberculosis
at pH 7.5 and 22°C
0.0003
morpholino(7-nitro-5-(trifluoromethyl)benzo[d]thiazol-2-yl)methanone
Mycobacterium tuberculosis
pH and temperature not specified in the publication
0.021
N,N-dimethyl-1-[1-[5-(1H-pyrrol-1-yl)-1,3,4-thiadiazol-2-yl]piperidine-4-carbonyl]piperidine-4-carboxamide
Mycobacterium tuberculosis
at pH 7.5 and 22°C
0.1
N-(pyridin-2-ylmethyl)-5-(trifluoromethyl)benzo[d]thiazole-2-carboxamide
Mycobacterium tuberculosis
IC50 above 0.1 mM, pH and temperature not specified in the publication
0.053
N-methyl-7-nitro-2-(piperidine-1-carbonyl)benzo[d]thiazole-5-carboxamide
Mycobacterium tuberculosis
pH and temperature not specified in the publication
0.000349
N-[(2S)-3-hydroxy-1-oxo-1-pyrrolidin-1-ylpropan-2-yl]-7-nitro-5-(trifluoromethyl)-1,3-benzothiazole-2-carboxamide
Mycobacterium tuberculosis
pH and temperature not specified in the publication
0.0004
[4-[(2H-1,3-benzodioxol-5-yl)methyl]piperazin-1-yl][1-[5-(1H-pyrrol-1-yl)-1,3,4-thiadiazol-2-yl]piperidin-4-yl]methanone
Mycobacterium tuberculosis
at pH 7.5 and 22°C
0.000054
[4-[(4-fluorophenyl)methyl]piperidin-1-yl][1-[5-(1H-pyrrol-1-yl)-1,3,4-thiadiazol-2-yl]piperidin-4-yl]methanone
Mycobacterium tuberculosis
at pH 7.5 and 22°C
0.1
[4-[(methylamino)methyl]piperidin-1-yl][1-[5-(1H-pyrrol-1-yl)-1,3,4-thiadiazol-2-yl]piperidin-4-yl]methanone
Mycobacterium tuberculosis
IC50 above 0.1 mM, at pH 7.5 and 22°C
0.0026
[4-[(pyridin-2-yl)methyl]piperidin-1-yl][1-[5-(1H-pyrrol-1-yl)-1,3,4-thiadiazol-2-yl]piperidin-4-yl]methanone
Mycobacterium tuberculosis
at pH 7.5 and 22°C
0.00044
[4-[(pyridin-3-yl)methyl]piperidin-1-yl][1-[5-(1H-pyrrol-1-yl)-1,3,4-thiadiazol-2-yl]piperidin-4-yl]methanone
Mycobacterium tuberculosis
at pH 7.5 and 22°C
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Trefzer, C.; Rengifo-Gonzalez, M.; Hinner, M.J.; Schneider, P.; Makarov, V.; Cole, S.T.; Johnsson, K.
Benzothiazinones: prodrugs that covalently modify the decaprenylphosphoryl-beta-D-ribose 2-epimerase DprE1 of Mycobacterium tuberculosis
J. Am. Chem. Soc.
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13663-13665
2010
Mycobacterium tuberculosis (P9WJF1), Mycobacterium tuberculosis, Mycobacterium tuberculosis H37Rv (P9WJF1)
brenda
Trefzer, C.; Skovierova, H.; Buroni, S.; Bobovska, A.; Nenci, S.; Molteni, E.; Pojer, F.; Pasca, M.; Makarov, V.; Cole, S.; Riccardi, G.; Mikusova, K.; Johnsson, K.
Benzothiazinones are suicide inhibitors of mycobacterial decaprenylphosphoryl-beta-D-ribofuranose 2'-oxidase DprE1
J. Am. Chem. Soc.
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912-915
2012
Mycolicibacterium smegmatis (A0R607)
brenda
Mikusova, K.; Huang, H.; Yagi, T.; Holsters, M.; Vereecke, D.; DHaeze, W.; Scherman, M.S.; Brennan, P.J.; McNeil, M.R.; Crick, D.C.
Decaprenylphosphoryl arabinofuranose, the donor of the D-arabinofuranosyl residues of mycobacterial arabinan, is formed via a two-step epimerization of decaprenylphosphoryl ribose
J. Bacteriol.
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8020-8025
2005
Mycobacterium tuberculosis (P9WJF1), Mycobacterium tuberculosis H37Rv (P9WJF1)
brenda
Crellin, P.K.; Brammananth, R.; Coppel, R.L.
Decaprenylphosphoryl-beta-D-ribose 2-epimerase, the target of benzothiazinones and dinitrobenzamides, is an essential enzyme in Mycobacterium smegmatis
PLoS ONE
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e16869
2011
Mycolicibacterium smegmatis (A0R607), Mycolicibacterium smegmatis
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Ribeiro, A.L.; Degiacomi, G.; Ewann, F.; Buroni, S.; Incandela, M.L.; Chiarelli, L.R.; Mori, G.; Kim, J.; Contreras-Dominguez, M.; Park, Y.S.; Han, S.J.; Brodin, P.; Valentini, G.; Rizzi, M.; Riccardi, G.; Pasca, M.R.
Analogous mechanisms of resistance to benzothiazinones and dinitrobenzamides in Mycobacterium smegmatis
PLoS ONE
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2011
Mycolicibacterium smegmatis (A0R607), Mycolicibacterium smegmatis
brenda
Christophe, T.; Jackson, M.; Hee, K.; Fenistein, D.; Contreras-Dominguez, M.; Kim, J.; Genovesio, A.; Carralot, J.; Ewann, F.; Kim, E.; Lee, S.; Kang, S.; Seo, M.; Eun, J.; Skovierova, H.; Pham, H.; Riccardi, G.; Youn, N.; Marsollier, L.; Kempf, M.; Jol
High content screening identifies decaprenyl-phosphoribose 2'-epimerase as a target for intracellular antimycobacterial inhibitors
PLoS Pathog.
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2009
Mycobacterium tuberculosis (P9WJF1), Mycobacterium tuberculosis H37Rv (P9WJF1)
brenda
Batt, S.M.; Jabeen, T.; Bhowruth, V.; Quill, L.; Lund, P.A.; Eggeling, L.; Alderwick, L.J.; Fuetterer, K.; Besra, G.S.
Structural basis of inhibition of Mycobacterium tuberculosis DprE1 by benzothiazinone inhibitors
Proc. Natl. Acad. Sci. USA
109
11354-11359
2012
Mycobacterium tuberculosis (P9WJF1), Mycobacterium tuberculosis, Mycobacterium tuberculosis H37Rv (P9WJF1)
brenda
Batt, S.M.; Cacho Izquierdo, M.; Castro Pichel, J.; Stubbs, C.J.; Vela-Glez Del Peral, L.; Perez-Herran, E.; Dhar, N.; Mouzon, B.; Rees, M.; Hutchinson, J.P.; Young, R.J.; McKinney, J.D.; Barros Aguirre, D.; Ballell, L.; Besra, G.S.; Argyrou, A.
Whole cell target engagement identifies novel inhibitors of Mycobacterium tuberculosis decaprenylphosphoryl-beta-D-ribose oxidase
ACS Infect. Dis.
1
615-626
2015
Mycobacterium tuberculosis (P9WJF1), Mycobacterium tuberculosis, Mycobacterium tuberculosis H37Rv (P9WJF1)
brenda
Makarov, V.; Neres, J.; Hartkoorn, R.C.; Ryabova, O.B.; Kazakova, E.; Sarkan, M.; Huszar, S.; Piton, J.; Kolly, G.S.; Vocat, A.; Conroy, T.M.; Mikusova, K.; Cole, S.T.
The 8-pyrrole-benzothiazinones are noncovalent inhibitors of DprE1 from Mycobacterium tuberculosis
Antimicrob. Agents Chemother.
59
4446-4452
2015
Mycobacterium tuberculosis (P9WJF1), Mycobacterium tuberculosis, Mycobacterium tuberculosis H37Rv (P9WJF1)
brenda
Foo, C.S.; Lechartier, B.; Kolly, G.S.; Boy-Roettger, S.; Neres, J.; Rybniker, J.; Lupien, A.; Sala, C.; Piton, J.; Cole, S.T.
Characterization of DprE1-mediated benzothiazinone resistance in Mycobacterium tuberculosis
Antimicrob. Agents Chemother.
60
6451-6459
2016
Mycobacterium tuberculosis (P9WJF1), Mycobacterium tuberculosis, Mycobacterium tuberculosis H37Rv (P9WJF1)
brenda
Riccardi, G.; Pasca, M.R.; Chiarelli, L.R.; Manina, G.; Mattevi, A.; Binda, C.
The DprE1 enzyme, one of the most vulnerable targets of Mycobacterium tuberculosis
Appl. Microbiol. Biotechnol.
97
8841-8848
2013
Mycobacterium tuberculosis
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Landge, S.; Mullick, A.B.; Nagalapur, K.; Neres, J.; Subbulakshmi, V.; Murugan, K.; Ghosh, A.; Sadler, C.; Fellows, M.D.; Humnabadkar, V.; Mahadevaswamy, J.; Vachaspati, P.; Sharma, S.; Kaur, P.; Mallya, M.; Rudrapatna, S.; Awasthy, D.; Sambandamurthy, V.K.; Pojer, F.; Cole, S.T.; Balganesh, T.S.; Ug, U.g.a.
Discovery of benzothiazoles as antimycobacterial agents: Synthesis, structure-activity relationships and binding studies with Mycobacterium tuberculosis decaprenylphosphoryl-beta-D-ribose 2'-oxidase
Bioorg. Med. Chem.
23
7694-7710
2015
Mycobacterium tuberculosis (P9WJF1)
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Panda, M.; Ramachandran, S.; Ramachandran, V.; Shirude, P.S.; Humnabadkar, V.; Nagalapur, K.; Sharma, S.; Kaur, P.; Guptha, S.; Narayan, A.; Mahadevaswamy, J.; Ambady, A.; Hegde, N.; Rudrapatna, S.S.; Hosagrahara, V.P.; Sambandamurthy, V.K.; Raichurkar, A.
Discovery of pyrazolopyridones as a novel class of noncovalent DprE1 inhibitor with potent anti-mycobacterial activity
J. Med. Chem.
57
4761-4771
2014
Mycobacterium tuberculosis (P9WJF1), Mycobacterium tuberculosis, Mycolicibacterium smegmatis (P9WJF1), Mycobacterium tuberculosis H37Rv (P9WJF1)
brenda
Naik, M.; Humnabadkar, V.; Tantry, S.J.; Panda, M.; Narayan, A.; Guptha, S.; Panduga, V.; Manjrekar, P.; Jena, L.K.; Koushik, K.; Shanbhag, G.; Jatheendranath, S.; Manjunatha, M.R.; Gorai, G.; Bathula, C.; Rudrapatna, S.; Achar, V.; Sharma, S.; Ambady, A.; Hegde, N.; Mahadevaswamy, J.; Kaur, P.; Samb, S.a.m.b.a.
4-aminoquinolone piperidine amides: noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity
J. Med. Chem.
57
5419-5434
2014
Mycobacterium tuberculosis (P9WJF1), Mycobacterium tuberculosis
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Bhutani, I.; Loharch, S.; Gupta, P.; Madathil, R.; Parkesh, R.
Structure, dynamics, and interaction of Mycobacterium tuberculosis (Mtb) DprE1 and DprE2 examined by molecular modeling, simulation, and electrostatic studies
PLoS ONE
10
e0119771
2015
Mycobacterium tuberculosis (P9WJF0), Mycobacterium tuberculosis (P9WJF1), Mycobacterium tuberculosis, Mycobacterium tuberculosis H37Rv (P9WJF1), Mycobacterium tuberculosis CDC 1551 (P9WJF0)
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Li, H.; Jogl, G.
Crystal structure of decaprenylphosphoryl-beta-D-ribose 2'-epimerase from Mycobacterium smegmatis
Proteins
81
538-543
2013
Mycolicibacterium smegmatis (A0R607), Mycolicibacterium smegmatis, Mycolicibacterium smegmatis ATCC 700084 (A0R607)
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Rogacki, M.K.; Pitta, E.; Balabon, O.; Huss, S.; Lopez-Roman, E.M.; Argyrou, A.; Blanco-Ruano, D.; Cacho, M.; Vande Velde, C.M.L.; Augustyns, K.; Ballell, L.; Barros, D.; Bates, R.H.; Cunningham, F.; Van der Veken, P.
Identification and profiling of hydantoins-A novel class of potent antimycobacterial DprE1 inhibitors
J. Med. Chem.
61
11221-11249
2018
Mycobacterium tuberculosis (P9WJF1), Mycobacterium tuberculosis, Mycobacterium tuberculosis H37Rv (P9WJF1)
brenda
Karabanovich, G.; Dusek, J.; Savkova, K.; Pavlis, O.; Pavkova, I.; Korabecny, J.; Kucera, T.; Kocova Vlckova, H.; Huszar, S.; Konyarikova, Z.; Konecna, K.; JandOurek, O.; Stolarkova, J.; Kordulakova, J.; Vavrova, K.; Pavek, P.
Development of 3,5-dinitrophenyl-containing 1,2,4-triazoles and their trifluoromethyl analogues as highly efficient antitubercular agents inhibiting decaprenylphosphoryl-beta-D-ribofuranose 2'-oxidase
J. Med. Chem.
62
8115-8139
2019
Mycobacterium tuberculosis (P9WJF1), Mycobacterium tuberculosis H37Rv (P9WJF1)
brenda