Inhibitors of bacterial enoyl acyl carrier protein reductase (FabI): 2,9-disubstituted 1,2,3,4-tetrahydropyrido[3,4-b]indoles as potential antibacterial agents.
An SAR study of a screening lead has led to the identification of 2,9-disubstituted 1,2,3,4-tetrahydropyrido[3,4-b]indoles as inhibitors of Staphylococcus aureus enoyl acyl carrier protein reductase (FabI).
Seefeld
M A
MA
GlaxoSmithKline Pharmaceuticals, Antimicrobial and Host Defense Division, 1250 S. Collegeville Road, Collegeville, PA 19426, USA. mark_a_seefeld@sbphrd.com
Miller
W H
WH
Newlander
K A
KA
Burgess
W J
WJ
Payne
D J
DJ
Rittenhouse
S F
SF
Moore
T D
TD
DeWolf
W E
WE
Keller
P M
PM
Qiu
X
X
Janson
C A
CA
Vaidya
K
K
Fosberry
A P
AP
Smyth
M G
MG
Jaworski
D D
DD
Slater-Radosti
C
C
Huffman
W F
WF
D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000494:pharmacology*; D050753:Enoyl-(Acyl-Carrier-Protein) Reductase (NADH); D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D004926:Escherichia coli / Q000187:drug effects; D029968:Escherichia coli Proteins; D054889:Fatty Acid Synthase, Type II; D020128:Inhibitory Concentration 50; D008826:Microbial Sensitivity Tests; D010088:Oxidoreductases / Q000037:antagonists & inhibitors*; D013211:Staphylococcus aureus / Q000187:drug effects; D013329:Structure-Activity Relationship; D014260:Triclosan / Q000494:pharmacology
D000900:Anti-Bacterial Agents; D004791:Enzyme Inhibitors; D029968:Escherichia coli Proteins; D014260:Triclosan; D010088:Oxidoreductases; D050753:Enoyl-(Acyl-Carrier-Protein) Reductase (NADH); C493924:fabI protein, E coli; D054889:Fatty Acid Synthase, Type II