Synthesis and antitubercular activity of 7-chloro-4-quinolinylhydrazones derivatives |
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Authors: | Andr L.P. Cand a, Marcelle de L. Ferreira, Karla C. Pais, Laura N.de F. Cardoso, Carlos R. Kaiser, Maria das Gra as M.de O. Henriques, Maria C.S. Louren o, Fl vio A.F.M. Bezerra,Marcus V.N. de Souza |
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Affiliation: | 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 |
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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. |
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Keywords: | Tuberculosis Quinoline Drugs |
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