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Literature summary for 2.3.1.180 extracted from

  • Castillo, Y.P.; Perez, M.A.
    Bacterial beta-ketoacyl-acyl carrier protein synthase III (FabH): an attractive target for the design of new broad-spectrum antimicrobial agents (2008), Mini Rev. Med. Chem., 8, 36-45.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(2R)-5-hydroxy-2,4-dimethyl-2-[(1E)-2-methylbuta-1,3-dien-1-yl]thiophen-3(2H)-one
-
Mycobacterium tuberculosis
(5R)-4-hydroxy-3,5-dimethyl-5-tetradecylthiophen-2(5H)-one
-
Mycobacterium tuberculosis
(5R)-4-hydroxy-3,5-dimethyl-5-tridecylthiophen-2(5H)-one
-
Mycobacterium tuberculosis
(5R)-4-hydroxy-5-[[4'-(hydroxymethyl)biphenyl-4-yl]methyl]-3,5-dimethylthiophen-2(5H)-one
-
Mycobacterium tuberculosis
(5R)-5-dodecyl-4-hydroxy-3,5-dimethylthiophen-2(5H)-one
-
Mycobacterium tuberculosis
(5R)-5-[3-(4-acetyl-3-hydroxyphenyl)prop-2-yn-1-yl]-4-hydroxy-3,5-dimethylthiophen-2(5H)-one
-
Mycobacterium tuberculosis
(5R)-5-[3-(4-acetylphenyl)prop-2-yn-1-yl]-4-hydroxy-3,5-dimethylthiophen-2(5H)-one
-
Mycobacterium tuberculosis
1-(4-carboxybutyl)-5-[(2,6-dichlorobenzyl)oxy]-1H-indole-2-carboxylic acid
-
Escherichia coli
1-(4-carboxybutyl)-5-[(2,6-dichlorobenzyl)oxy]-1H-indole-2-carboxylic acid
-
Haemophilus influenzae
1-[(6-chloro-1,3-benzodioxol-5-yl)methyl]-5-[(2,6-dichlorobenzyl)oxy]-1H-indole-2-carboxylic acid
-
Escherichia coli
1-[(6-chloro-1,3-benzodioxol-5-yl)methyl]-5-[(2,6-dichlorobenzyl)oxy]-1H-indole-2-carboxylic acid
-
Haemophilus influenzae
2-([[4-(3,5-dimethylpiperidin-1-yl)-3-phenoxyphenyl]carbonyl]amino)benzoic acid
-
Escherichia coli
2-hydroxy-6-[[(2-phenoxybiphenyl-4-yl)carbonyl]amino]benzoic acid
-
Enterococcus faecium
2-hydroxy-6-[[(2-phenoxybiphenyl-4-yl)carbonyl]amino]benzoic acid
-
Escherichia coli
2-hydroxy-6-[[(2-phenoxybiphenyl-4-yl)carbonyl]amino]benzoic acid
-
Haemophilus influenzae
2-hydroxy-6-[[(2-phenoxybiphenyl-4-yl)carbonyl]amino]benzoic acid
-
Neisseria meningitidis
2-hydroxy-6-[[(2-phenoxybiphenyl-4-yl)carbonyl]amino]benzoic acid
-
Staphylococcus aureus
2-hydroxy-6-[[(2-phenoxybiphenyl-4-yl)carbonyl]amino]benzoic acid
-
Streptococcus pneumoniae
2-hydroxy-6-[[(2-phenoxybiphenyl-4-yl)carbonyl]amino]benzoic acid
-
Streptococcus pyogenes
2-[[(3-phenoxy-4-piperidin-1-ylphenyl)carbonyl]amino]benzoic acid
-
Escherichia coli
2-[[(3-phenoxy-4-thiomorpholin-4-ylphenyl)carbonyl]amino]benzoic acid
-
Escherichia coli
2-[[(4'-fluoro-3'-methyl-2-phenoxybiphenyl-4-yl)carbonyl]amino]-6-hydroxybenzoic acid
-
Enterococcus faecium
2-[[(4'-fluoro-3'-methyl-2-phenoxybiphenyl-4-yl)carbonyl]amino]-6-hydroxybenzoic acid
-
Escherichia coli
2-[[(4'-fluoro-3'-methyl-2-phenoxybiphenyl-4-yl)carbonyl]amino]-6-hydroxybenzoic acid
-
Neisseria meningitidis
2-[[(4'-fluoro-3'-methyl-2-phenoxybiphenyl-4-yl)carbonyl]amino]-6-hydroxybenzoic acid
-
Staphylococcus aureus
2-[[(4'-fluoro-3'-methyl-2-phenoxybiphenyl-4-yl)carbonyl]amino]-6-hydroxybenzoic acid
-
Streptococcus pneumoniae
2-[[(4'-fluoro-3'-methyl-2-phenoxybiphenyl-4-yl)carbonyl]amino]-6-hydroxybenzoic acid
-
Streptococcus pyogenes
4,5-dichloro-3H-1,2-dithiol-3-one
-
Staphylococcus aureus
4,5-dichloro-3H-1,2-dithiole-3-thione
-
Staphylococcus aureus
5-chloro-4-phenyl-3H-1,2-dithiol-3-one
-
Staphylococcus aureus
thiolactomycin
-
Escherichia coli
thiolactomycin
-
Haemophilus influenzae
thiolactomycin
-
Streptococcus pneumoniae

Organism

Organism UniProt Comment Textmining
Enterococcus faecium
-
-
-
Escherichia coli
-
-
-
Haemophilus influenzae
-
-
-
Mycobacterium tuberculosis
-
-
-
Neisseria meningitidis
-
-
-
Pseudomonas aeruginosa
-
-
-
Staphylococcus aureus
-
-
-
Streptococcus pneumoniae
-
-
-
Streptococcus pyogenes
-
-
-

Synonyms

Synonyms Comment Organism
ecFabH
-
Escherichia coli
efFabH
-
Enterococcus faecium
hiFabH
-
Haemophilus influenzae
mtFabH
-
Mycobacterium tuberculosis
nmFabH
-
Neisseria meningitidis
paFabH
-
Pseudomonas aeruginosa
saFabH
-
Staphylococcus aureus
spFabH
-
Streptococcus pneumoniae
spyFabH
-
Streptococcus pneumoniae
spyFabH
-
Streptococcus pyogenes

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000004
-
-
Streptococcus pyogenes 2-hydroxy-6-[[(2-phenoxybiphenyl-4-yl)carbonyl]amino]benzoic acid
0.000004
-
-
Enterococcus faecium 2-hydroxy-6-[[(2-phenoxybiphenyl-4-yl)carbonyl]amino]benzoic acid
0.00004
-
-
Haemophilus influenzae 1-[(6-chloro-1,3-benzodioxol-5-yl)methyl]-5-[(2,6-dichlorobenzyl)oxy]-1H-indole-2-carboxylic acid
0.00014
-
-
Escherichia coli 1-(4-carboxybutyl)-5-[(2,6-dichlorobenzyl)oxy]-1H-indole-2-carboxylic acid
0.00088
-
-
Escherichia coli 1-[(6-chloro-1,3-benzodioxol-5-yl)methyl]-5-[(2,6-dichlorobenzyl)oxy]-1H-indole-2-carboxylic acid
0.001
-
-
Escherichia coli 2-[[(3-phenoxy-4-thiomorpholin-4-ylphenyl)carbonyl]amino]benzoic acid
0.0014
-
-
Escherichia coli 2-hydroxy-6-[[(2-phenoxybiphenyl-4-yl)carbonyl]amino]benzoic acid
0.00192
-
-
Staphylococcus aureus 5-chloro-4-phenyl-3H-1,2-dithiol-3-one
0.002
-
-
Escherichia coli 2-[[(3-phenoxy-4-piperidin-1-ylphenyl)carbonyl]amino]benzoic acid
0.00225
-
-
Staphylococcus aureus 4,5-dichloro-3H-1,2-dithiol-3-one
0.0024
-
-
Haemophilus influenzae 2-hydroxy-6-[[(2-phenoxybiphenyl-4-yl)carbonyl]amino]benzoic acid
0.00319
-
-
Staphylococcus aureus 4,5-dichloro-3H-1,2-dithiole-3-thione
0.0038
-
-
Staphylococcus aureus 2-hydroxy-6-[[(2-phenoxybiphenyl-4-yl)carbonyl]amino]benzoic acid
0.00404
-
-
Mycobacterium tuberculosis (5R)-5-[3-(4-acetylphenyl)prop-2-yn-1-yl]-4-hydroxy-3,5-dimethylthiophen-2(5H)-one
0.0057
-
-
Escherichia coli 2-([[4-(3,5-dimethylpiperidin-1-yl)-3-phenoxyphenyl]carbonyl]amino)benzoic acid
0.007
-
-
Haemophilus influenzae 1-(4-carboxybutyl)-5-[(2,6-dichlorobenzyl)oxy]-1H-indole-2-carboxylic acid
0.00702
-
-
Mycobacterium tuberculosis (5R)-5-[3-(4-acetyl-3-hydroxyphenyl)prop-2-yn-1-yl]-4-hydroxy-3,5-dimethylthiophen-2(5H)-one
0.017
-
-
Mycobacterium tuberculosis (5R)-4-hydroxy-5-[[4'-(hydroxymethyl)biphenyl-4-yl]methyl]-3,5-dimethylthiophen-2(5H)-one
0.019
-
-
Mycobacterium tuberculosis (5R)-4-hydroxy-5-[[4'-(hydroxymethyl)biphenyl-4-yl]methyl]-3,5-dimethylthiophen-2(5H)-one
0.04
-
-
Mycobacterium tuberculosis (5R)-5-dodecyl-4-hydroxy-3,5-dimethylthiophen-2(5H)-one
0.08
-
-
Mycobacterium tuberculosis (5R)-4-hydroxy-3,5-dimethyl-5-tetradecylthiophen-2(5H)-one
0.08
-
-
Mycobacterium tuberculosis (5R)-4-hydroxy-3,5-dimethyl-5-tridecylthiophen-2(5H)-one
0.11
-
-
Escherichia coli thiolactomycin