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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.

Activities of Rifamycin Derivatives against Wild-Type and rpoB Mutants of Chlamydia trachomatis

Minsheng Xia,1 Robert J. Suchland,1 Joli A. Carswell,1 John Van Duzer,2 Debra K. Buxton,2 Kara Brown,2 David M. Rothstein,2 and Walter E. Stamm1*

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.


* Corresponding author. Mailing address: 1959 NE Pacific Street, University of Washington, Box 356523, Seattle, WA 98195. Phone: (206) 616-4170. Fax: (206) 616-4898. E-mail: wes{at}u.washington.edu.


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.




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