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.
Publication types
-
Research Support, U.S. Gov't, P.H.S.
MeSH terms
-
Antitubercular Agents / chemical synthesis*
-
Antitubercular Agents / chemistry
-
Antitubercular Agents / pharmacology
-
Microbial Sensitivity Tests
-
Mycobacterium tuberculosis / drug effects
-
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
Substances
-
9-(ethylcarboxymethyl)-6-(decylthio)-9H-purine
-
9-(ethylcarboxymethyl)-6-(dodecylthio)-9H-purine
-
Antitubercular Agents
-
Purines
-
Pyridines
-
Pyrimidines
-
Sulfides