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Synthesis and antitubercular activity of 7-chloro-4-quinolinylhydrazones derivatives. 2009
André L P Candéa, and
Marcelle de L Ferreira, and
Karla C Pais, and
Laura N de F Cardoso, and
Carlos R Kaiser, and
Maria das Graças M de O Henriques, and
Maria C S Lourenço, and
Flávio A F M Bezerra, and
Marcus V N de Souza
FioCruz-Fundação Oswaldo Cruz, Instituto de Tecnologia em Fármacos-Far Manguinhos. Rua Sizenando Nabuco, 100, Manguinhos, 21041-250 Rio de Janeiro, RJ, Brazil.
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 H(37)Rv. The compounds 3f, 3i and 3o were non-cytotoxic and exhibited an important minimum inhibitory concentration (MIC) activity (2.5 microg/mL), which can be compared with that of the first line drugs, ethambutol (3.12 microg/mL) and rifampicin (2.0 microg/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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