Synthesis and anti-mycobacterial activity of ( E)- N′-(monosubstituted-benzylidene)isonicotinohydrazide derivatives

A series of 22 ( E)- N′-(monosubstituted-benzylidene)isonicotinohydrazide derivatives have been synthesized and evaluated for their in vitro antibacterial activity against Mycobacterium tuberculosis H 37Rv using Alamar Blue susceptibility test and the activity expressed as the minimum inhibitory con...

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Bibliographic Details
Published in:European journal of medicinal chemistry 2008-06, Vol.43 (6), p.1344-1347
Main Authors: Lourenço, Maria Cristina da Silva, Ferreira, Marcelle de Lima, de Souza, Marcus Vinícius Nora, Peralta, Mônica Amado, Vasconcelos, Thatyana Rocha Alves, Henriques, Maria das Graças M.O.
Format: Article
Language:English
Subjects:
Anti-mycobacterial
Antibacterial agents
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antitubercular Agents - chemical synthesis
Antitubercular Agents - pharmacology
Biological and medical sciences
Derivatives
Hydrazines - chemical synthesis
Hydrazines - pharmacology
Isoniazid
Magnetic Resonance Spectroscopy
Medical sciences
Mycobacterium tuberculosis
Mycobacterium tuberculosis - drug effects
Pharmacology. Drug treatments
Spectrophotometry, Infrared
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Summary:A series of 22 ( E)- N′-(monosubstituted-benzylidene)isonicotinohydrazide derivatives have been synthesized and evaluated for their in vitro antibacterial activity against Mycobacterium tuberculosis H 37Rv using Alamar Blue susceptibility test and the activity expressed as the minimum inhibitory concentration (MIC) in μg/mL. Compounds 2f, 2g, 2j, 2k and 2q exhibited a significant activity (0.31–0.62 μg/mL) when compared with first line drugs such as isoniazid (INH) and rifampicin (RIP) and could be a good starting point to develop new lead compounds in the fight against multi-drug resistant tuberculosis. A series of 22 N'-[( E)-(monosubstituted-phenyl)methylidene]isonicotinohydrazide derivatives ( 2a– v) have been synthesized and evaluated for their in vitro antibacterial activity against Mycobacterium tuberculosis H 37Rv using the Alamar Blue susceptibility test. ▪
ISSN:0223-5234
1768-3254
DOI:10.1016/j.ejmech.2007.08.003