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Literature summary for 2.3.1.180 extracted from

  • Li, J.R.; Li, D.D.; Wang, R.R.; Sun, J.; Dong, J.J.; Du, Q.R.; Fang, F.; Zhang, W.M.; Zhu, H.L.
    Design and synthesis of thiazole derivatives as potent FabH inhibitors with antibacterial activity (2014), Eur. J. Med. Chem., 75, 438-447.
    View publication on PubMed
Search for more literature for 2.3.1.180

Cloned(Commentary)

Cloned (Comment) Organism
gene fabH, recombinant His-tagged enzyme expression in Escherichia coli strain BL21(DE3) Escherichia coli

Inhibitors

Inhibitors Comment Organism Structure
3-bromo-N-(4-phenyl-1,3-thiazol-2-yl)benzamide
-
 Escherichia coli
3-bromo-N-[4-(4-bromophenyl)-1,3-thiazol-2-yl]benzamide fitting 3-bromo-N-[4-(4-bromophenyl)-1,3-thiazol-2-yl]benzamide into the active site of Escherichia coli FabH,PDB ID 3IL9 Escherichia coli
3-chloro-N-(4-phenyl-1,3-thiazol-2-yl)benzamide
-
 Escherichia coli
3-ethoxy-N-(4-phenyl-1,3-thiazol-2-yl)benzamide
-
 Escherichia coli
3-methoxy-N-(4-phenyl-1,3-thiazol-2-yl)benzamide
-
 Escherichia coli
4-bromo-N-(4-phenyl-1,3-thiazol-2-yl)benzamide
-
 Escherichia coli
4-bromo-N-[4-(4-bromophenyl)-1,3-thiazol-2-yl]benzamide
-
 Escherichia coli
4-chloro-N-(4-phenyl-1,3-thiazol-2-yl)benzamide
-
 Escherichia coli
4-fluoro-N-(4-phenyl-1,3-thiazol-2-yl)benzamide
-
 Escherichia coli
kanamycin B
-
 Escherichia coli
additional information design and synthesis of thiazole derivatives as potent FabH inhibitors with antibacterial activity, MIC values, docking simulation and structure-activity relationsship study, binding mode, overview Escherichia coli
N-(4-phenyl-1,3-thiazol-2-yl)-5,8-dihydronaphthalene-2-carboxamide
-
 Escherichia coli
N-(4-phenyl-1,3-thiazol-2-yl)benzamide
-
 Escherichia coli
N-(4-phenyl-1,3-thiazol-2-yl)morpholine-4-carboxamide
-
 Escherichia coli
N-(4-phenyl-1,3-thiazol-2-yl)naphthalene-1-carboxamide
-
 Escherichia coli
N-[4-(4-bromophenyl)-1,3-thiazol-2-yl]-3-chlorobenzamide
-
 Escherichia coli
N-[4-(4-bromophenyl)-1,3-thiazol-2-yl]-3-ethoxybenzamide
-
 Escherichia coli
N-[4-(4-bromophenyl)-1,3-thiazol-2-yl]-3-methoxybenzamide
-
 Escherichia coli
N-[4-(4-bromophenyl)-1,3-thiazol-2-yl]-4-chlorobenzamide
-
 Escherichia coli
N-[4-(4-bromophenyl)-1,3-thiazol-2-yl]-4-fluorobenzamide
-
 Escherichia coli
N-[4-(4-bromophenyl)-1,3-thiazol-2-yl]-5,8-dihydronaphthalene-2-carboxamide
-
 Escherichia coli
N-[4-(4-bromophenyl)-1,3-thiazol-2-yl]benzamide
-
 Escherichia coli
N-[4-(4-bromophenyl)-1,3-thiazol-2-yl]morpholine-4-carboxamide
-
 Escherichia coli
N-[4-(4-bromophenyl)-1,3-thiazol-2-yl]naphthalene-1-carboxamide
-
 Escherichia coli
penicillin G fitting penicillin G into the active site of Escherichia coli FabH, PDB ID 3IL9 Escherichia coli

Metals/Ions

Metals/Ions Comment Organism Structure
Mg2+ required Escherichia coli

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
acetyl-CoA + a malonyl-[acyl-carrier protein] Escherichia coli
-
 an acetoacetyl-[acyl-carrier protein] + CoA + CO2
-
 ?

Organism

Organism UniProt Comment Textmining
Escherichia coli P0A6R0 gene fabH
-

Purification (Commentary)

Purification (Comment) Organism
recombinant His-tagged enzyme from Escherichia coli strain BL21(DE3) by nickel affinity chromatography and dialysis Escherichia coli

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
acetyl-CoA + a malonyl-[acyl-carrier protein]
-
 Escherichia coli an acetoacetyl-[acyl-carrier protein] + CoA + CO2
-
 ?

Synonyms

Synonyms Comment Organism
FabH
-
 Escherichia coli

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
 assay at Escherichia coli

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7
-
 assay at Escherichia coli

Cofactor

Cofactor Comment Organism Structure
acetyl-CoA
-
 Escherichia coli

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0049
-
 pH 7.0, 37°C Escherichia coli penicillin G
0.0058
-
 pH 7.0, 37°C, recombinant His-tagged enzyme Escherichia coli 3-bromo-N-[4-(4-bromophenyl)-1,3-thiazol-2-yl]benzamide
0.0066
-
 pH 7.0, 37°C, recombinant His-tagged enzyme Escherichia coli N-[4-(4-bromophenyl)-1,3-thiazol-2-yl]-3-methoxybenzamide
0.0093
-
 pH 7.0, 37°C, recombinant His-tagged enzyme Escherichia coli N-[4-(4-bromophenyl)-1,3-thiazol-2-yl]-3-chlorobenzamide
0.0123
-
 pH 7.0, 37°C, recombinant His-tagged enzyme Escherichia coli 3-chloro-N-(4-phenyl-1,3-thiazol-2-yl)benzamide
0.0269
-
 pH 7.0, 37°C, recombinant His-tagged enzyme Escherichia coli 3-bromo-N-(4-phenyl-1,3-thiazol-2-yl)benzamide
0.0293
-
 pH 7.0, 37°C, recombinant His-tagged enzyme Escherichia coli N-[4-(4-bromophenyl)-1,3-thiazol-2-yl]-4-fluorobenzamide
0.0347
-
 pH 7.0, 37°C, recombinant His-tagged enzyme Escherichia coli N-[4-(4-bromophenyl)-1,3-thiazol-2-yl]-4-chlorobenzamide
0.0384
-
 pH 7.0, 37°C, recombinant His-tagged enzyme Escherichia coli 4-fluoro-N-(4-phenyl-1,3-thiazol-2-yl)benzamide
0.0418
-
 pH 7.0, 37°C, recombinant His-tagged enzyme Escherichia coli 4-chloro-N-(4-phenyl-1,3-thiazol-2-yl)benzamide
0.0481
-
 pH 7.0, 37°C, recombinant His-tagged enzyme Escherichia coli 4-bromo-N-[4-(4-bromophenyl)-1,3-thiazol-2-yl]benzamide
0.1
-
 above, pH 7.0, 37°C, recombinant His-tagged enzyme Escherichia coli N-(4-phenyl-1,3-thiazol-2-yl)benzamide
0.1
-
 above, pH 7.0, 37°C, recombinant His-tagged enzyme Escherichia coli N-[4-(4-bromophenyl)-1,3-thiazol-2-yl]benzamide

General Information

General Information Comment Organism
metabolism enzyme FabH catalyzes the initiation reaction of fatty acid biosynthesis Escherichia coli