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Literature summary extracted from

  • Al-Balas, Q.; Anthony, N.G.; Al-Jaidi, B.; Alnimr, A.; Abbott, G.; Brown, A.K.; Taylor, R.C.; Besra, G.S.; McHugh, T.D.; Gillespie, S.H.; Johnston, B.F.; Mackay, S.P.; Coxon, G.D.
    Identification of 2-aminothiazole-4-carboxylate derivatives active against Mycobacterium tuberculosis H37Rv and the beta-ketoacyl-ACP synthase mtFabH (2009), PLoS ONE, 4, e5617.
    View publication on PubMedView publication on EuropePMC

Application

EC Number Application Comment Organism
2.3.1.180 drug development the enzyme is a target for inhibitor development Mycobacterium tuberculosis

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.3.1.180 2-amino-5-(3-chlorophenyl)thiazole-4-carboxylic acid MIC value is 0.125 mM Mycobacterium tuberculosis
2.3.1.180 2-amino-5-methylthiazole-4-carboxylic acid MIC value is 0.00035 mM Mycobacterium tuberculosis
2.3.1.180 4'-[(3-hydroxy-2,4-dimethyl-5-oxo-2,5-dihydrothiophen-2-yl)methyl]biphenyl-4-carboxylic acid
-
 Mycobacterium tuberculosis
2.3.1.180 5-benzyl-2-(2-bromoacetamido)thiazole-4-carboxylic acid
-
 Mycobacterium tuberculosis
2.3.1.180 methyl 2-(2-bromoacetamido)-5-(3-chlorophenyl) thiazole-4-carboxylate
-
 Mycobacterium tuberculosis
2.3.1.180 methyl 2-(2-bromoacetamido)-5-phenylthiazole-4-carboxylate
-
 Mycobacterium tuberculosis
2.3.1.180 methyl 2-amino-5-benzylthiazole-4-carboxylate MIC value is 240 nM Mycobacterium tuberculosis
2.3.1.180 methyl 2-amino-5-methylthiazole-4-carboxylate MIC value is 0.093 mM Mycobacterium tuberculosis
2.3.1.180 methyl 5-benzyl-2-(2-bromoacetamido)thiazole-4-carboxylate
-
 Mycobacterium tuberculosis
2.3.1.180 additional information modeling studies of binding of 2-aminothiazole-4-carboxylate analogues to FabH, overview Mycobacterium tuberculosis
2.3.1.180 thiolactomycin
-
 Mycobacterium tuberculosis

Organism

EC Number Organism UniProt Comment Textmining
2.3.1.180 Mycobacterium tuberculosis P9WNG3
-
-
2.3.1.180 Mycobacterium tuberculosis H37Rv P9WNG3
-
-

Synonyms

EC Number Synonyms Comment Organism
2.3.1.180 beta-ketoacyl-ACP synthase
-
 Mycobacterium tuberculosis
2.3.1.180 FabH
-
 Mycobacterium tuberculosis

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.3.1.180 0.00243
-
-
 Mycobacterium tuberculosis methyl 2-(2-bromoacetamido)-5-(3-chlorophenyl) thiazole-4-carboxylate
2.3.1.180 0.003
-
-
 Mycobacterium tuberculosis 4'-[(3-hydroxy-2,4-dimethyl-5-oxo-2,5-dihydrothiophen-2-yl)methyl]biphenyl-4-carboxylic acid
2.3.1.180 0.0032
-
-
 Mycobacterium tuberculosis methyl 2-(2-bromoacetamido)-5-phenylthiazole-4-carboxylate
2.3.1.180 0.075
-
-
 Mycobacterium tuberculosis thiolactomycin
2.3.1.180 0.1598
-
-
 Mycobacterium tuberculosis methyl 5-benzyl-2-(2-bromoacetamido)thiazole-4-carboxylate
2.3.1.180 0.718
-
-
 Mycobacterium tuberculosis 5-benzyl-2-(2-bromoacetamido)thiazole-4-carboxylic acid