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

M A Seefeld; W H Miller; K A Newlander; W J Burgess; D J Payne; S F Rittenhouse; T D Moore; W E DeWolf Jr; P M Keller; X Qiu; C A Janson; K Vaidya; A P Fosberry; M G Smyth; D D Jaworski; C Slater-Radosti; W F Huffman

doi:10.1016/s0960-894x(01)00405-x

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

Bioorg Med Chem Lett. 2001 Sep 3;11(17):2241-4. doi: 10.1016/s0960-894x(01)00405-x.

Authors

M A Seefeld¹, W H Miller, K A Newlander, W J Burgess, D J Payne, S F Rittenhouse, T D Moore, W E DeWolf Jr, P M Keller, X Qiu, C A Janson, K Vaidya, A P Fosberry, M G Smyth, D D Jaworski, C Slater-Radosti, W F Huffman

Affiliation

¹ GlaxoSmithKline Pharmaceuticals, Antimicrobial and Host Defense Division, 1250 S. Collegeville Road, Collegeville, PA 19426, USA. [email protected]

PMID: 11527706
DOI: 10.1016/s0960-894x(01)00405-x

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).

MeSH terms

Anti-Bacterial Agents / chemistry
Anti-Bacterial Agents / pharmacology*
Enoyl-(Acyl-Carrier-Protein) Reductase (NADH)
Enzyme Inhibitors / chemistry*
Enzyme Inhibitors / pharmacology*
Escherichia coli / drug effects
Escherichia coli Proteins
Fatty Acid Synthase, Type II
Inhibitory Concentration 50
Microbial Sensitivity Tests
Oxidoreductases / antagonists & inhibitors*
Staphylococcus aureus / drug effects
Structure-Activity Relationship
Triclosan / pharmacology

Substances

Anti-Bacterial Agents
Enzyme Inhibitors
Escherichia coli Proteins
Triclosan
Oxidoreductases
Enoyl-(Acyl-Carrier-Protein) Reductase (NADH)
fabI protein, E coli
Fatty Acid Synthase, Type II

Associated data

PDB/1I30