Synthesis and Antimycobacterial Activity of 6-Arylpurines: The Requirements for the N-9 Substituent in Active Antimycobacterial Purines
- 6 February 2002
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 45 (6), 1383-1386
- https://doi.org/10.1021/jm0110284
Abstract
6-Arylpurines carrying a variety of substituents in the 9-position were prepared by Stille coupling between appropriately substituted 6-chloropurines and aryl(tributyl)tin, and the compounds were screened for antibacterial activity against Mycobacterium tuberculosis H37Rv. The lowest minimum inhibitory concentration value, 0.78 μg/mL, was found for 9-benzyl-2-chloro-6-(2-furyl)purine. This compound exhibited relatively low cytotoxicity, and it was active against several singly drug-resistant strains of M. tuberculosis.Keywords
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