1,4-Disubstituted imidazoles are potential antibacterial agents functioning as inhibitors of enoyl acyl carrier protein reductase (FabI).
1,4-Disubstituted imidazole inhibitors of Staphylococcus aureus and Escherichia coli enoyl acyl carrier protein reductase (FabI) have been identified. Crystal structure data shows the inhibitor 1 bound in the enzyme active site of E. coli FabI.
Heerding
D A
DA
GlaxoSmithKline Pharmaceuticals, Antibacterials and Host Defense, 1250 S. Collegeville Road, Collegeville, PA 19426, USA. dirk_a_heerding@sbphrd.com
Chan
G
G
DeWolf
W E
WE
Fosberry
A P
AP
Janson
C A
CA
Jaworski
D D
DD
McManus
E
E
Miller
W H
WH
Moore
T D
TD
Payne
D J
DJ
Qiu
X
X
Rittenhouse
S F
SF
Slater-Radosti
C
C
Smith
W
W
Takata
D T
DT
Vaidya
K S
KS
Yuan
C C
CC
Huffman
W F
WF
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D050753:Enoyl-(Acyl-Carrier-Protein) Reductase (NADH); D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D004926:Escherichia coli / Q000187:drug effects; D029968:Escherichia coli Proteins; D054889:Fatty Acid Synthase, Type II; D007093:Imidazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests; D010088:Oxidoreductases / Q000037:antagonists & inhibitors*; D013211:Staphylococcus aureus / Q000187:drug effects
D000900:Anti-Bacterial Agents; D004791:Enzyme Inhibitors; D029968:Escherichia coli Proteins; D007093:Imidazoles; D010088:Oxidoreductases; D050753:Enoyl-(Acyl-Carrier-Protein) Reductase (NADH); C493924:fabI protein, E coli; D054889:Fatty Acid Synthase, Type II