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Literature summary for 2.3.1.180 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

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

Inhibitors

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

Organism

Organism UniProt Comment Textmining
Mycobacterium tuberculosis P9WNG3
-
-
Mycobacterium tuberculosis H37Rv P9WNG3
-
-

Synonyms

Synonyms Comment Organism
beta-ketoacyl-ACP synthase
-
Mycobacterium tuberculosis
FabH
-
Mycobacterium tuberculosis

IC50 Value

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