title: 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.
abstract: 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).
authors.affiliation: GlaxoSmithKline Pharmaceuticals, Antimicrobial and Host Defense Division, 1250 S. Collegeville Road, Collegeville, PA 19426, USA. mark_a_seefeld@sbphrd.com
authors.forename: M A
authors.initials: MA
authors.lastname: Seefeld
authors.forename: W H
authors.initials: WH
authors.lastname: Miller
authors.forename: K A
authors.initials: KA
authors.lastname: Newlander
authors.forename: W J
authors.initials: WJ
authors.lastname: Burgess
authors.forename: D J
authors.initials: DJ
authors.lastname: Payne
authors.forename: S F
authors.initials: SF
authors.lastname: Rittenhouse
authors.forename: T D
authors.initials: TD
authors.lastname: Moore
authors.forename: W E
authors.initials: WE
authors.lastname: DeWolf
authors.forename: P M
authors.initials: PM
authors.lastname: Keller
authors.forename: X
authors.initials: X
authors.lastname: Qiu
authors.forename: C A
authors.initials: CA
authors.lastname: Janson
authors.forename: K
authors.initials: K
authors.lastname: Vaidya
authors.forename: A P
authors.initials: AP
authors.lastname: Fosberry
authors.forename: M G
authors.initials: MG
authors.lastname: Smyth
authors.forename: D D
authors.initials: DD
authors.lastname: Jaworski
authors.forename: C
authors.initials: C
authors.lastname: Slater-Radosti
authors.forename: W F
authors.initials: WF
authors.lastname: Huffman
mesh_terms: 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
chemical_list: 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