Synthesis and in vitro activity of 6-amino-2,9-diarylpurines for Mycobacterium tuberculosis

A mild method was developed to synthesize 6-amino-2-phenolic-9-alkyl and 9-arylpurines. The new compounds were screened for antibacterial activity against Mycobacterium tuberculosis strain H(37)Rv. The 9-tolyl derivatives with a dimethylamino or a piperidine substituent in C6 and the 3-hydroxyphenyl or 4-hydroxyphenyl substituent in C2 were highly active against the bacilli. (C) 2009 Elsevier Ltd. All rights reserved.Antimycobacterial data were provided by the Tuberculosis Antimicrobial Acquisition and Coordinating Facility (TAACF) through a research and development contract with the US National Institute of Allergy and Infectious Diseases. The authors gratefully acknowledge the financial support by Universidade do Minho, Centro de Quimica and Fundacao para a Ciencia e Tecnologia (project PPCDT/QUI/59356/2004 and a PhD grant to C.C. SFRH/BD/22270/2005)