Synthesis and antitubercular activity of 7-chloro-4-quinolinylhydrazones derivatives.
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.
Candéa
André L P
AL
FioCruz-Fundação Oswaldo Cruz, Instituto de Tecnologia em Fármacos-Far Manguinhos. Rua Sizenando Nabuco, 100, Manguinhos, 21041-250 Rio de Janeiro, RJ, Brazil.
Ferreira
Marcelle de L
Mde L
Pais
Karla C
KC
Cardoso
Laura N de F
LN
Kaiser
Carlos R
CR
Henriques
Maria das Graças M de O
Md
Lourenço
Maria C S
MC
Bezerra
Flávio A F M
FA
de Souza
Marcus V N
MV
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D000995:Antitubercular Agents / Q000138:chemical synthesis*; D004977:Ethambutol / Q000494:pharmacology; D006801:Humans; D008826:Microbial Sensitivity Tests; D050296:Microbial Viability / Q000187:drug effects; D009169:Mycobacterium tuberculosis / Q000187:drug effects; D021281:Quantitative Structure-Activity Relationship; D012293:Rifampin / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014376:Tuberculosis / Q000188:drug therapy
D000900:Anti-Bacterial Agents; D000995:Antitubercular Agents; D004977:Ethambutol; D012293:Rifampin