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Synthesis and Antimycobacterial Activity of 6-Arylpurines:  The Requirements for the N-9 Substituent in Active Antimycobacterial Purines

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journal contribution
posted on 06.02.2002 by Lise-Lotte Gundersen, Jon Nissen-Meyer, Bjørn Spilsberg
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.