Literature summary for 3.5.1.108 extracted from

Tomaras, A.; McPherson, C.; Kuhn, M.; Carif, A.; Mullins, L.; George, D.; Desbonnet, C.; Eidem, T.; Montgomery, J.; Brown, M.; Reilly, U.; Miller, A.; O'Donnell, J.
LpxC Inhibitors as new antibacterial agents and tools for studying regulation of lipid a biosynthesis in Gram-negative pathogens (2014), mBio, 5, e01551-14.

Search for more literature for 3.5.1.108

Inhibitors

Inhibitors	Comment	Organism	Structure
(2R)-4-([1,1'-biphenyl]-4-yl)-N-hydroxy-2-(methanesulfonyl)-2-methylbutanamide	-	Acinetobacter baumannii
(2R)-4-([1,1'-biphenyl]-4-yl)-N-hydroxy-2-(methanesulfonyl)-2-methylbutanamide	-	Klebsiella pneumoniae
(2R)-4-([1,1'-biphenyl]-4-yl)-N-hydroxy-2-(methanesulfonyl)-2-methylbutanamide	-	Pseudomonas aeruginosa
(2R)-4-[4-(2-fluoro-4-methoxyphenyl)-2-oxopyridin-1(2H)-yl]-N-hydroxy-2-(methanesulfonyl)-2-methylbutanamide	-	Acinetobacter baumannii
(2R)-4-[4-(2-fluoro-4-methoxyphenyl)-2-oxopyridin-1(2H)-yl]-N-hydroxy-2-(methanesulfonyl)-2-methylbutanamide	-	Klebsiella pneumoniae
(2R)-4-[4-(2-fluoro-4-methoxyphenyl)-2-oxopyridin-1(2H)-yl]-N-hydroxy-2-(methanesulfonyl)-2-methylbutanamide	-	Pseudomonas aeruginosa
(2R)-N-hydroxy-2-(methanesulfonyl)-2-methyl-4-(2-oxo-4-phenylpyridin-1(2H)-yl)butanamide	-	Acinetobacter baumannii
(2R)-N-hydroxy-2-(methanesulfonyl)-2-methyl-4-(2-oxo-4-phenylpyridin-1(2H)-yl)butanamide	-	Klebsiella pneumoniae
(2R)-N-hydroxy-2-(methanesulfonyl)-2-methyl-4-(2-oxo-4-phenylpyridin-1(2H)-yl)butanamide	-	Pseudomonas aeruginosa
meropenem	-	Acinetobacter baumannii
meropenem	-	Klebsiella pneumoniae
meropenem	-	Pseudomonas aeruginosa
additional information	evaluation of LpxC inhibitors that are potent and rapidly bactericidal against multiple Gram-negative species, overview	Acinetobacter baumannii
additional information	evaluation of LpxC inhibitors that are potent and rapidly bactericidal against multiple Gram-negative species, overview	Klebsiella pneumoniae
additional information	evaluation of LpxC inhibitors that are potent and rapidly bactericidal against multiple Gram-negative species, overview	Pseudomonas aeruginosa
N-[(2S,3R)-3-hydroxy-1-(hydroxyamino)-1-oxobutan-2-yl]-4-({4-[(morpholin-4-yl)methyl]phenyl}ethynyl)benzamide	-	Acinetobacter baumannii
N-[(2S,3R)-3-hydroxy-1-(hydroxyamino)-1-oxobutan-2-yl]-4-({4-[(morpholin-4-yl)methyl]phenyl}ethynyl)benzamide	-	Klebsiella pneumoniae
N-[(2S,3R)-3-hydroxy-1-(hydroxyamino)-1-oxobutan-2-yl]-4-({4-[(morpholin-4-yl)methyl]phenyl}ethynyl)benzamide	-	Pseudomonas aeruginosa

Organism

Organism	UniProt	Comment	Textmining
Acinetobacter baumannii	-	different isolates, gene lpxC	-
Klebsiella pneumoniae	-	different isolates, gene lpxC	-
Pseudomonas aeruginosa	-	and different isolates, gene lpxC	-

Synonyms

Synonyms	Comment	Organism
LpxC	-	Pseudomonas aeruginosa
LpxC	-	Klebsiella pneumoniae
LpxC	-	Acinetobacter baumannii

Temperature Optimum [°C]

Temperature Optimum [°C]	Temperature Optimum Maximum [°C]	Comment	Organism
37	-	assay at	Pseudomonas aeruginosa
37	-	assay at	Klebsiella pneumoniae
37	-	assay at	Acinetobacter baumannii

pH Optimum

pH Optimum Minimum	pH Optimum Maximum	Comment	Organism
7.4	-	assay at	Pseudomonas aeruginosa
7.4	-	assay at	Klebsiella pneumoniae
7.4	-	assay at	Acinetobacter baumannii

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.000000069	-	pH 7.4, 37°C	Klebsiella pneumoniae	(2R)-4-[4-(2-fluoro-4-methoxyphenyl)-2-oxopyridin-1(2H)-yl]-N-hydroxy-2-(methanesulfonyl)-2-methylbutanamide
0.00000068	-	pH 7.4, 37°C	Klebsiella pneumoniae	(2R)-N-hydroxy-2-(methanesulfonyl)-2-methyl-4-(2-oxo-4-phenylpyridin-1(2H)-yl)butanamide
0.000001	-	pH 7.4, 37°C	Klebsiella pneumoniae	(2R)-4-([1,1'-biphenyl]-4-yl)-N-hydroxy-2-(methanesulfonyl)-2-methylbutanamide
0.0000011	-	wild-type, pH 7.4, 37°C	Pseudomonas aeruginosa	(2R)-4-[4-(2-fluoro-4-methoxyphenyl)-2-oxopyridin-1(2H)-yl]-N-hydroxy-2-(methanesulfonyl)-2-methylbutanamide
0.0000014	-	wild-type, pH 7.4, 37°C	Pseudomonas aeruginosa	(2R)-4-([1,1'-biphenyl]-4-yl)-N-hydroxy-2-(methanesulfonyl)-2-methylbutanamide
0.0000021	-	mutant M62R, pH 7.4, 37°C	Pseudomonas aeruginosa	(2R)-4-[4-(2-fluoro-4-methoxyphenyl)-2-oxopyridin-1(2H)-yl]-N-hydroxy-2-(methanesulfonyl)-2-methylbutanamide
0.0000028	-	mutant M62R, pH 7.4, 37°C	Pseudomonas aeruginosa	(2R)-N-hydroxy-2-(methanesulfonyl)-2-methyl-4-(2-oxo-4-phenylpyridin-1(2H)-yl)butanamide
0.0000036	-	wild-type, pH 7.4, 37°C	Pseudomonas aeruginosa	(2R)-N-hydroxy-2-(methanesulfonyl)-2-methyl-4-(2-oxo-4-phenylpyridin-1(2H)-yl)butanamide
0.0000079	-	mutant M62R, pH 7.4, 37°C	Pseudomonas aeruginosa	(2R)-4-([1,1'-biphenyl]-4-yl)-N-hydroxy-2-(methanesulfonyl)-2-methylbutanamide
0.000041	-	pH 7.4, 37°C	Acinetobacter baumannii	(2R)-4-([1,1'-biphenyl]-4-yl)-N-hydroxy-2-(methanesulfonyl)-2-methylbutanamide
0.00011	-	pH 7.4, 37°C	Acinetobacter baumannii	(2R)-N-hydroxy-2-(methanesulfonyl)-2-methyl-4-(2-oxo-4-phenylpyridin-1(2H)-yl)butanamide
0.000183	-	pH 7.4, 37°C	Acinetobacter baumannii	(2R)-4-[4-(2-fluoro-4-methoxyphenyl)-2-oxopyridin-1(2H)-yl]-N-hydroxy-2-(methanesulfonyl)-2-methylbutanamide

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Release 2023.1 (January 2023)