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Literature summary for 2.3.1.180 extracted from

  • Lv, P.C.; Wang, K.R.; Yang, Y.; Mao, W.J.; Chen, J.; Xiong, J.; Zhu, H.L.
    Design, synthesis and biological evaluation of novel thiazole derivatives as potent FabH inhibitors (2009), Bioorg. Med. Chem. Lett., 19, 6750-6754.
    View publication on PubMed

Application

Application Comment Organism
drug development FabH is a particularly attractive target for design of antibacterial agents since it is central to the initiation of fatty acid biosynthesis and is highly conserved among Gram positive and negative bacteria Escherichia coli

Inhibitors

Inhibitors Comment Organism Structure
2,4-dibromo-6-[(E)-[(4-phenyl-1,3-thiazol-2-yl)hydrazono]methyl]phenol
-
Escherichia coli
2,4-dibromo-6-[(E)-[[4-(3,4-dichlorophenyl)-1,3-thiazol-2-yl]hydrazono]methyl]phenol
-
Escherichia coli
2,4-dibromo-6-[(E)-[[4-(4-chlorophenyl)-1,3-thiazol-2-yl]hydrazono]methyl]phenol
-
Escherichia coli
2,4-dichloro-6-[(E)-[(4-phenyl-1,3-thiazol-2-yl)hydrazono]methyl]phenol
-
Escherichia coli
2,4-dichloro-6-[(E)-[[4-(3,4-dichlorophenyl)-1,3-thiazol-2-yl]hydrazono]methyl]phenol
-
Escherichia coli
2,4-dichloro-6-[(E)-[[4-(4-chlorophenyl)-1,3-thiazol-2-yl]hydrazono]methyl]phenol
-
Escherichia coli
2-[(2E)-2-[(4-bromophenyl)methylidene]hydrazino]-4-(3,4-dichlorophenyl)-1,3-thiazole
-
Escherichia coli
2-[(2E)-2-[(4-bromophenyl)methylidene]hydrazino]-4-(4-chlorophenyl)-1,3-thiazole
-
Escherichia coli
2-[(2E)-2-[(4-bromophenyl)methylidene]hydrazino]-4-phenyl-1,3-thiazole
-
Escherichia coli
2-[(2E)-2-[(4-chlorophenyl)methylidene]hydrazino]-4-(3,4-dichlorophenyl)-1,3-thiazole
-
Escherichia coli
2-[(2E)-2-[(4-chlorophenyl)methylidene]hydrazino]-4-phenyl-1,3-thiazole
-
Escherichia coli
2-[(2E)-2-[(4-fluorophenyl)methylidene]hydrazino]-4-phenyl-1,3-thiazole
-
Escherichia coli
2-[(2E)-2-[(4-methoxyphenyl)methylidene]hydrazino]-4-phenyl-1,3-thiazole
-
Escherichia coli
2-[(2E)-2-[(4-methylphenyl)methylidene]hydrazino]-4-phenyl-1,3-thiazole
-
Escherichia coli
4-(3,4-dichlorophenyl)-2-[(2E)-2-[(4-fluorophenyl)methylidene]hydrazino]-1,3-thiazole
-
Escherichia coli
4-(3,4-dichlorophenyl)-2-[(2E)-2-[(4-methoxyphenyl)methylidene]hydrazino]-1,3-thiazole
-
Escherichia coli
4-(3,4-dichlorophenyl)-2-[(2E)-2-[(4-methylphenyl)methylidene]hydrazino]-1,3-thiazole
-
Escherichia coli
4-(4-chlorophenyl)-2-[(2E)-2-[(4-chlorophenyl)methylidene]hydrazino]-1,3-thiazole
-
Escherichia coli
4-(4-chlorophenyl)-2-[(2E)-2-[(4-fluorophenyl)methylidene]hydrazino]-1,3-thiazole
-
Escherichia coli
4-(4-chlorophenyl)-2-[(2E)-2-[(4-methoxyphenyl)methylidene]hydrazino]-1,3-thiazole
-
Escherichia coli
4-(4-chlorophenyl)-2-[(2E)-2-[(4-methylphenyl)methylidene]hydrazino]-1,3-thiazole
-
Escherichia coli
4-bromo-2-[(E)-[(4-phenyl-1,3-thiazol-2-yl)hydrazono]methyl]phenol
-
Escherichia coli
4-bromo-2-[(E)-[[4-(3,4-dichlorophenyl)-1,3-thiazol-2-yl]hydrazono]methyl]phenol
-
Escherichia coli
4-bromo-2-[(E)-[[4-(4-chlorophenyl)-1,3-thiazol-2-yl]hydrazono]methyl]phenol
-
Escherichia coli
4-chloro-2-[(E)-[(4-phenyl-1,3-thiazol-2-yl)hydrazono]methyl]phenol
-
Escherichia coli
4-chloro-2-[(E)-[[4-(3,4-dichlorophenyl)-1,3-thiazol-2-yl]hydrazono]methyl]phenol
-
Escherichia coli
4-chloro-2-[(E)-[[4-(4-chlorophenyl)-1,3-thiazol-2-yl]hydrazono]methyl]phenol
-
Escherichia coli
additional information inhibitor design and synthesis, analysis of inhibitory potencies against FabH and antibacterial activities, overview Escherichia coli

Organism

Organism UniProt Comment Textmining
Escherichia coli
-
gene fabH
-

Synonyms

Synonyms Comment Organism
ACP synthase III
-
Escherichia coli
beta-ketoacylacylcarrier protein synthase III
-
Escherichia coli
FabH
-
Escherichia coli

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0036
-
-
Escherichia coli 2,4-dibromo-6-[(E)-[[4-(3,4-dichlorophenyl)-1,3-thiazol-2-yl]hydrazono]methyl]phenol
0.0068
-
-
Escherichia coli 4-bromo-2-[(E)-[[4-(4-chlorophenyl)-1,3-thiazol-2-yl]hydrazono]methyl]phenol
0.0117
-
-
Escherichia coli 4-chloro-2-[(E)-[[4-(4-chlorophenyl)-1,3-thiazol-2-yl]hydrazono]methyl]phenol
0.0165
-
-
Escherichia coli 2,4-dichloro-6-[(E)-[[4-(3,4-dichlorophenyl)-1,3-thiazol-2-yl]hydrazono]methyl]phenol
0.0396
-
-
Escherichia coli 4-chloro-2-[(E)-[[4-(3,4-dichlorophenyl)-1,3-thiazol-2-yl]hydrazono]methyl]phenol
0.0434
-
-
Escherichia coli 4-bromo-2-[(E)-[[4-(3,4-dichlorophenyl)-1,3-thiazol-2-yl]hydrazono]methyl]phenol
0.0576
-
-
Escherichia coli 2,4-dichloro-6-[(E)-[[4-(4-chlorophenyl)-1,3-thiazol-2-yl]hydrazono]methyl]phenol
0.0784
-
-
Escherichia coli 2,4-dibromo-6-[(E)-[[4-(4-chlorophenyl)-1,3-thiazol-2-yl]hydrazono]methyl]phenol

General Information

General Information Comment Organism
physiological function FabH is central to the initiation of fatty acid biosynthesis Escherichia coli