title: Activities of rifamycin derivatives against wild-type and rpoB mutants of Chlamydia trachomatis.
abstract: Rifalazil, a semisynthetic rifamycin, was shown previously to have exceptional potency against Chlamydia trachomatis (MIC of 0.00025 microg/ml). We therefore tested 250 additional rifamycin derivatives and identified 12 with activities that are eightfold more potent than that of rifalazil. These compounds also showed exceptional activities against rifampin-resistant strains that carry missense mutations in the rpoB gene. The antimicrobial potency and intracellular penetration of these agents suggest their potential in treatment of chlamydial infections.
authors.affiliation: Division of Infectious Diseases, Department of Medicine, University of Washington, Seattle, WA 98195, USA.
authors.forename: Minsheng
authors.initials: M
authors.lastname: Xia
authors.forename: Robert J
authors.initials: RJ
authors.lastname: Suchland
authors.forename: Joli A
authors.initials: JA
authors.lastname: Carswell
authors.forename: John
authors.initials: J
authors.lastname: Van Duzer
authors.forename: Debra K
authors.initials: DK
authors.lastname: Buxton
authors.forename: Kara
authors.initials: K
authors.lastname: Brown
authors.forename: David M
authors.initials: DM
authors.lastname: Rothstein
authors.forename: Walter E
authors.initials: WE
authors.lastname: Stamm
mesh_terms: D000900:Anti-Bacterial Agents / Q000494:pharmacology*; D002690:Chlamydia Infections / Q000382:microbiology; D002692:Chlamydia trachomatis / Q000187:drug effects* / Q000235:genetics*; D006801:Humans; D020125:Mutation, Missense; D012294:Rifamycins / Q000494:pharmacology*
chemical_list: D000900:Anti-Bacterial Agents; D012294:Rifamycins; C068980:KRM 1648