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Antimicrobial Agents and Chemotherapy, September 2005, p. 3974-3976, Vol. 49, No. 9
0066-4804/05/$08.00+0 doi:10.1128/AAC.49.9.3974-3976.2005
Copyright © 2005, American Society for Microbiology. All Rights Reserved.
Division of Infectious Diseases, Department of Medicine, University of Washington, Seattle, Washington 98195,1 ActivBiotics, Inc., Lexington, Massachusetts 024212
Received 1 February 2005/ Returned for modification 28 February 2005/ Accepted 25 April 2005
Rifalazil, a semisynthetic rifamycin, was shown previously to have exceptional potency against Chlamydia trachomatis (MIC of 0.00025 µg/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.
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