title: Synthesis and antitubercular activity of 7-chloro-4-quinolinylhydrazones derivatives.
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 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.
authors.affiliation: FioCruz-Fundação Oswaldo Cruz, Instituto de Tecnologia em Fármacos-Far Manguinhos. Rua Sizenando Nabuco, 100, Manguinhos, 21041-250 Rio de Janeiro, RJ, Brazil.
authors.forename: André L P
authors.initials: AL
authors.lastname: Candéa
authors.forename: Marcelle de L
authors.initials: Mde L
authors.lastname: Ferreira
authors.forename: Karla C
authors.initials: KC
authors.lastname: Pais
authors.forename: Laura N de F
authors.initials: LN
authors.lastname: Cardoso
authors.forename: Carlos R
authors.initials: CR
authors.lastname: Kaiser
authors.forename: Maria das Graças M de O
authors.initials: Md
authors.lastname: Henriques
authors.forename: Maria C S
authors.initials: MC
authors.lastname: Lourenço
authors.forename: Flávio A F M
authors.initials: FA
authors.lastname: Bezerra
authors.forename: Marcus V N
authors.initials: MV
authors.lastname: de Souza
mesh_terms: 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
chemical_list: D000900:Anti-Bacterial Agents; D000995:Antitubercular Agents; D004977:Ethambutol; D012293:Rifampin