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Synthesis and antitubercular activity of 7-chloro-4-quinolinylhydrazones derivatives |
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| Authors: | Andr LP Canda Marcelle de L Ferreira Karla C Pais Laura Nde F Cardoso Carlos R Kaiser Maria das Graas Mde O Henriques Maria CS Loureno Flvio AFM Bezerra Marcus VN de Souza |
| Institution: | aFioCruz-Fundação Oswaldo Cruz, Instituto de Tecnologia em Fármacos-Far Manguinhos. Rua Sizenando Nabuco, 100, Manguinhos, 21041-250 Rio de Janeiro, RJ, Brazil;bDepartamento de Química Orgânica, Instituto de Química, Universidade Federal do Rio de Janeiro, CP 68563, 21945-970 Rio de Janeiro, Brazil;cInstituto de Pesquisas Clínica Evandro Chagas, IPEC, Av. Brasil, 4365 Manguinhos, Rio de Janeiro, Brazil |
| Abstract: | A series of twenty-one 7-chloro-4-quinolinylhydrazones (3a–u) have been synthesized and evaluated for their in vitro antibacterial activity against Mycobacterium tuberculosis H37Rv. The compounds 3f, 3i and 3o were non-cytotoxic and exhibited an important minimum inhibitory concentration (MIC) activity (2.5 μg/mL), which can be compared with that of the first line drugs, ethambutol (3.12 μg/mL) and rifampicin (2.0 μg/mL). These results can be considered an important start point for the rational design of new leads for anti-TB compounds. |
| Keywords: | Tuberculosis Quinoline Drugs |
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