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  • Title: Antimycobacterial agents. 1. Thio analogues of purine.
    Author: Pathak AK, Pathak V, Seitz LE, Suling WJ, Reynolds RC.
    Journal: J Med Chem; 2004 Jan 01; 47(1):273-6. PubMed ID: 14695841.
    Abstract:
    Thio analogues of purine, pyridine, and pyrimidine were prepared based on the initial activity screening of several analogues of these heterocycles against Mycobacterium tuberculosis (Mtb). Certain 6-thio-substituted purine analogues described herein showed moderate to good inhibitory activity. In particular, two purine analogues 9-(ethylcarboxymethyl)-6-(decylthio)-9H-purine (20) and 9-(ethylcarboxymethyl)-6-(dodecylthio)-9H-purine (21) exhibited MIC values of 1.56 and 0.78 microg/mL respectively against the Mtb H(37)Rv strain. N(9)-Substitution apparently enhances the antimycobacterial activity in the purine series described herein.
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