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Literature summary 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

Cloned(Commentary)

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

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.3.1.180 3-bromo-N-(4-phenyl-1,3-thiazol-2-yl)benzamide
-
 Escherichia coli
2.3.1.180 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
2.3.1.180 3-chloro-N-(4-phenyl-1,3-thiazol-2-yl)benzamide
-
 Escherichia coli
2.3.1.180 3-ethoxy-N-(4-phenyl-1,3-thiazol-2-yl)benzamide
-
 Escherichia coli
2.3.1.180 3-methoxy-N-(4-phenyl-1,3-thiazol-2-yl)benzamide
-
 Escherichia coli
2.3.1.180 4-bromo-N-(4-phenyl-1,3-thiazol-2-yl)benzamide
-
 Escherichia coli
2.3.1.180 4-bromo-N-[4-(4-bromophenyl)-1,3-thiazol-2-yl]benzamide
-
 Escherichia coli
2.3.1.180 4-chloro-N-(4-phenyl-1,3-thiazol-2-yl)benzamide
-
 Escherichia coli
2.3.1.180 4-fluoro-N-(4-phenyl-1,3-thiazol-2-yl)benzamide
-
 Escherichia coli
2.3.1.180 kanamycin B
-
 Escherichia coli
2.3.1.180 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
2.3.1.180 N-(4-phenyl-1,3-thiazol-2-yl)-5,8-dihydronaphthalene-2-carboxamide
-
 Escherichia coli
2.3.1.180 N-(4-phenyl-1,3-thiazol-2-yl)benzamide
-
 Escherichia coli
2.3.1.180 N-(4-phenyl-1,3-thiazol-2-yl)morpholine-4-carboxamide
-
 Escherichia coli
2.3.1.180 N-(4-phenyl-1,3-thiazol-2-yl)naphthalene-1-carboxamide
-
 Escherichia coli
2.3.1.180 N-[4-(4-bromophenyl)-1,3-thiazol-2-yl]-3-chlorobenzamide
-
 Escherichia coli
2.3.1.180 N-[4-(4-bromophenyl)-1,3-thiazol-2-yl]-3-ethoxybenzamide
-
 Escherichia coli
2.3.1.180 N-[4-(4-bromophenyl)-1,3-thiazol-2-yl]-3-methoxybenzamide
-
 Escherichia coli
2.3.1.180 N-[4-(4-bromophenyl)-1,3-thiazol-2-yl]-4-chlorobenzamide
-
 Escherichia coli
2.3.1.180 N-[4-(4-bromophenyl)-1,3-thiazol-2-yl]-4-fluorobenzamide
-
 Escherichia coli
2.3.1.180 N-[4-(4-bromophenyl)-1,3-thiazol-2-yl]-5,8-dihydronaphthalene-2-carboxamide
-
 Escherichia coli
2.3.1.180 N-[4-(4-bromophenyl)-1,3-thiazol-2-yl]benzamide
-
 Escherichia coli
2.3.1.180 N-[4-(4-bromophenyl)-1,3-thiazol-2-yl]morpholine-4-carboxamide
-
 Escherichia coli
2.3.1.180 N-[4-(4-bromophenyl)-1,3-thiazol-2-yl]naphthalene-1-carboxamide
-
 Escherichia coli
2.3.1.180 penicillin G fitting penicillin G into the active site of Escherichia coli FabH, PDB ID 3IL9 Escherichia coli

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
2.3.1.180 Mg2+ required Escherichia coli

Natural Substrates/ Products (Substrates)

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

Organism

EC Number Organism UniProt Comment Textmining
2.3.1.180 Escherichia coli P0A6R0 gene fabH
-

Purification (Commentary)

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

Substrates and Products (Substrate)

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

Synonyms

EC Number Synonyms Comment Organism
2.3.1.180 FabH
-
 Escherichia coli

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
2.3.1.180 37
-
 assay at Escherichia coli

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
2.3.1.180 7
-
 assay at Escherichia coli

Cofactor

EC Number Cofactor Comment Organism Structure
2.3.1.180 acetyl-CoA
-
 Escherichia coli

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.3.1.180 0.0049
-
 pH 7.0, 37°C Escherichia coli penicillin G
2.3.1.180 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
2.3.1.180 0.0066
-
 pH 7.0, 37°C, recombinant His-tagged enzyme Escherichia coli N-[4-(4-bromophenyl)-1,3-thiazol-2-yl]-3-methoxybenzamide
2.3.1.180 0.0093
-
 pH 7.0, 37°C, recombinant His-tagged enzyme Escherichia coli N-[4-(4-bromophenyl)-1,3-thiazol-2-yl]-3-chlorobenzamide
2.3.1.180 0.0123
-
 pH 7.0, 37°C, recombinant His-tagged enzyme Escherichia coli 3-chloro-N-(4-phenyl-1,3-thiazol-2-yl)benzamide
2.3.1.180 0.0269
-
 pH 7.0, 37°C, recombinant His-tagged enzyme Escherichia coli 3-bromo-N-(4-phenyl-1,3-thiazol-2-yl)benzamide
2.3.1.180 0.0293
-
 pH 7.0, 37°C, recombinant His-tagged enzyme Escherichia coli N-[4-(4-bromophenyl)-1,3-thiazol-2-yl]-4-fluorobenzamide
2.3.1.180 0.0347
-
 pH 7.0, 37°C, recombinant His-tagged enzyme Escherichia coli N-[4-(4-bromophenyl)-1,3-thiazol-2-yl]-4-chlorobenzamide
2.3.1.180 0.0384
-
 pH 7.0, 37°C, recombinant His-tagged enzyme Escherichia coli 4-fluoro-N-(4-phenyl-1,3-thiazol-2-yl)benzamide
2.3.1.180 0.0418
-
 pH 7.0, 37°C, recombinant His-tagged enzyme Escherichia coli 4-chloro-N-(4-phenyl-1,3-thiazol-2-yl)benzamide
2.3.1.180 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
2.3.1.180 0.1
-
 above, pH 7.0, 37°C, recombinant His-tagged enzyme Escherichia coli N-(4-phenyl-1,3-thiazol-2-yl)benzamide
2.3.1.180 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

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