Synthesis and antitubercular activity of heteroaromatic isonicotinoyl and 7-chloro-4-quinolinyl hydrazone derivatives.
Two series of N'-(E)-heteroaromatic-isonicotinohydrazide derivatives (3a-f and 4a-b) and 1-(7-chloroquinolin-4-yl)-2-[(heteroaromatic)methylene]hydrazone derivatives (5a-f and 6a-b) have been synthesized and evaluated for their in vitro antibacterial activity against Mycobacterium tuberculosis H37Rv. Several compounds were noncytotoxic and exhibited significant minimum inhibitory concentration (MIC) activity (3.12, 2.50, 1.25, or 0.60 microg/mL), which can be compared to that of the first-line drugs ethambutol (3.12 microg/mL) and rifampicin (2.0 microg/ml). These results can be considered an important starting point for the rational design of new leads for anti-TB compounds.
Ferreira
Marcelle de L
Mde L
FioCruz-Fundação Oswaldo Cruz, Instituto de Tecnologia em Fármacos-Far Manguinhos, Manguinhos, Rio de Janeiro.
Gonçalves
Raoni S B
RS
Cardoso
Laura N de F
LN
Kaiser
Carlos R
CR
Candea
Andre L P
AL
Henriques
Maria das Graças M de O
Md
Lourenço
Maria C S
MC
Bezerra
Flavio A F M
FA
de Souza
Marcus V N
MV
D000995:Antitubercular Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D006835:Hydrazones / Q000138:chemical synthesis* / Q000494:pharmacology*; D009682:Magnetic Resonance Spectroscopy; D008826:Microbial Sensitivity Tests; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D021241:Spectrometry, Mass, Electrospray Ionization
D000995:Antitubercular Agents; D006835:Hydrazones