Activities of rifamycin derivatives against wild-type and rpoB mutants of Chlamydia trachomatis.
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.
Xia
Minsheng
M
Division of Infectious Diseases, Department of Medicine, University of Washington, Seattle, WA 98195, USA.
Suchland
Robert J
RJ
Carswell
Joli A
JA
Van Duzer
John
J
Buxton
Debra K
DK
Brown
Kara
K
Rothstein
David M
DM
Stamm
Walter E
WE
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*
D000900:Anti-Bacterial Agents; D012294:Rifamycins; C068980:KRM 1648