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Antimicrobial Agents and Chemotherapy, February 2007, p. 752-754, Vol. 51, No. 2
0066-4804/07/$08.00+0 doi:10.1128/AAC.01369-06
Copyright © 2007, American Society for Microbiology. All Rights Reserved.
Infectious Diseases Division, Kaplan Medical Center, The Hebrew University and Hadassah Jerusalem, Rehovot, Israel,1 Department of Microbiology and Immunology, Howard Hughes Medical Institute, Albert Einstein College of Medicine, Bronx, New York,2 Department of Chemistry, State University of New York at Albany, Albany, New York3
Received 2 November 2006/ Accepted 4 November 2006
The activity of different analogs of pyrazinamide on Mycobacterium tuberculosis fatty acid synthase type I (FASI) in replicating bacilli was studied. Palmitic acid biosynthesis was diminished by 96% in bacilli treated with n-propyl pyrazinoate, 94% in bacilli treated with 5-chloro-pyrazinamide, and 97% in bacilli treated with pyrazinoic acid, the pharmacologically active agent of pyrazinamide. We conclude that the minimal structure of pyrazine ring with an acyl group is sufficient for FASI inhibition and antimycobacterial activity.
Published ahead of print on 13 November 2006.
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