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Bioorg Med Chem. 2013 Apr 1;21(7):1685-95. doi: 10.1016/j.bmc.2013.01.054. Epub 2013 Feb 4.

6-Oxo and 6-thio purine analogs as antimycobacterial agents.

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  • 1Drug Discovery Division, Southern Research Institute, 2000 9th Avenue South, Birmingham, AL 35205, USA.


6-Oxo and 6-thio analogs of purine were prepared based on the initial activity screening of a small, diverse purine library against Mycobacterium tuberculosis (Mtb). Certain 6-oxo and 6-thio-substituted purine analogs described herein showed moderate to good inhibitory activity. N(9)-substitution apparently enhances the anti-mycobacterial activity in the purine series described herein. Several 2-amino and 2-chloro purine analogs were also synthesized that showed moderate inhibitory activity against Mtb.

Copyright © 2013 Elsevier Ltd. All rights reserved.

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