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Synthesis and antitubercular evaluation of 7-chloro-4-alkoxyquinoline derivatives

Marcelle de Lima Ferreira Bispo, Laura Nogueira de Faria Cardoso, Maria C. S. Lourenço, Flávio Augusto Ferreira Martins Bezerra, Rodrigo Pedro Pinto Soares Pinto Soares, Caryne Margotto Bertollo, Marcus Vinícius Nora de Souza


A series of eight 7-chloro-4-alkoxyquinoline derivatives (2a-h) have been synthesized and their in vitro (antimycobacterial) activity against Mycobacterium tuberculosis was evaluated.  Furthermore, all the active compounds were selected for evaluation of their cytotoxicities against the human hepatoma (HepG2) and the relative selectivity (selective index) of these compounds against M. tuberculosis compared to HepG2 was calculated based on MLD50/MIC ratios.  These biological results have been compared to a series of 7-chloro-4-aminoquinoline derivatives 1a-i, previously identified by our research group with the aim to provide important information about the structure-activity relationship of quinoline derivatives.

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