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Synthesis and antimycobacterial activity of N'-[(E)-(monosubstituted-benzylidene)]-2-pyrazinecarbohydrazide derivatives.
Vergara, Fátima M F; Lima, Camilo H da S; Henriques, Maria das Graças M de O; Candéa, André L P; Lourenço, Maria C S; Ferreira, Marcelle de L; Kaiser, Carlos R; de Souza, Marcus V N.
Afiliación
  • Vergara FM; Fundação Oswaldo Cruz, Instituto de Tecnologia em Fármacos-Far Manguinhos, Fundação Oswaldo Cruz, 21041-250, Rio de Janeiro, RJ, Brazil.
Eur J Med Chem ; 44(12): 4954-9, 2009 Dec.
Article en En | MEDLINE | ID: mdl-19765866
The present article describes a series of twenty-six N'-[(E)-(monosubstituted-benzylidene)]-2-pyrazinecarbohydrazide (4-29), which were synthesized and evaluated for their cell viabilities in non infected and infected macrophages with Mycobacterium bovis Bacillus Calmette-Guerin (BCG). Afterwards, the non-cytotoxic compounds (4, 6, 8, 15, 21, 23, 24, 27 and 28) were assessed against Mycobacterium tuberculosis ATCC 27294 using the micro plate Alamar Blue assay (MABA) and the activity expressed as the minimum inhibitory concentration (MIC) in microg/mL. The compounds 6, 23, 27 and 28 exhibited a significant activity (50-100 microg/mL) when compared with first line drugs such as pyrazinamide and were not cytotoxic in their respective MIC values.
Asunto(s)

Texto completo: 1 Colección: 01-internacional Banco de datos: MEDLINE Asunto principal: Pirazinamida / Compuestos de Bencilideno / Hidrazinas / Antibacterianos / Mycobacterium tuberculosis / Antituberculosos Límite: Humans Idioma: En Revista: Eur J Med Chem Año: 2009 Tipo del documento: Article País de afiliación: Brasil

Texto completo: 1 Colección: 01-internacional Banco de datos: MEDLINE Asunto principal: Pirazinamida / Compuestos de Bencilideno / Hidrazinas / Antibacterianos / Mycobacterium tuberculosis / Antituberculosos Límite: Humans Idioma: En Revista: Eur J Med Chem Año: 2009 Tipo del documento: Article País de afiliación: Brasil