Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10593057 | Bioorganic & Medicinal Chemistry Letters | 2013 | 8 Pages |
Abstract
During the course of our research to find novel mode of action antibacterials, we discovered a series of hydroxyl tricyclic compounds that showed good potency against Gram-positive and Gram-negative pathogens. These compounds inhibit bacterial type IIA topoisomerases. Herein we will discuss structure-activity relationships in this series and report advanced studies on compound 1 (GSK966587) which demonstrates good PK and in vivo efficacy properties. X-ray crystallographic studies were used to provide insight into the structural basis for the difference in antibacterial potency between enantiomers.
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Timothy J. Miles, Alan J. Hennessy, Ben Bax, Gerald Brooks, Barry S. Brown, Pamela Brown, Nathalie Cailleau, Dongzhao Chen, Steven Dabbs, David T. Davies, Joel M. Esken, Ilaria Giordano, Jennifer L. Hoover, Jianzhong Huang, Graham E. Jones,