Antimycobacterial agents. 1. Thio analogues of purine.

Antimycobacterial agents. 1. Thio analogues of purine.
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DOI:
10.1021/jm030389b
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发表时间:
2004
影响因子:
7.3
通讯作者:
A. Pathak;V. Pathak;Lainne E. Seitz;W. J. Suling;R. Reynolds
A. Pathak;V. Pathak;Lainne E. Seitz;W. J. Suling;R. Reynolds
中科院分区:
医学1区
文献类型:
--
作者:
A. Pathak;V. Pathak;Lainne E. Seitz;W. J. Suling;R. Reynolds

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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.