Antimycobacterial Agents. 1. Thio Analogues of Purine

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 p...

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Bibliographic Details
Published in:Journal of medicinal chemistry 2004-01, Vol.47 (1), p.273-276
Main Authors: Pathak, Ashish K, Pathak, Vibha, Seitz, Lainne E, Suling, William J, Reynolds, Robert C
Format: Article
Language:English
Subjects:
Antibacterial agents
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antitubercular Agents - chemical synthesis
Antitubercular Agents - chemistry
Antitubercular Agents - pharmacology
Biological and medical sciences
Medical sciences
Microbial Sensitivity Tests
Mycobacterium tuberculosis - drug effects
Pharmacology. Drug treatments
Purines - chemical synthesis
Purines - chemistry
Purines - pharmacology
Pyridines - chemical synthesis
Pyridines - chemistry
Pyridines - pharmacology
Pyrimidines - chemical synthesis
Pyrimidines - chemistry
Pyrimidines - pharmacology
Sulfides - chemical synthesis
Sulfides - chemistry
Sulfides - pharmacology
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Summary: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 μg/mL respectively against the Mtb H37Rv strain. N9-Substitution apparently enhances the antimycobacterial activity in the purine series described herein.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm030389b