Details

Autor(en) / Beteiligte

• 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.

Titel

Synthesis and antimycobacterial activity of N′-[( E)-(monosubstituted-benzylidene)]-2-pyrazinecarbohydrazide derivatives

Ist Teil von

• European journal of medicinal chemistry, 2009-12, Vol.44 (12), p.4954-4959

Ort / Verlag

Kidlington: Elsevier Masson SAS

Erscheinungsjahr

2009

Quelle

MEDLINE

Beschreibungen/Notizen

• 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 μg/mL. The compounds 6, 23, 27 and 28 exhibited a significant activity (50–100 μg/mL) when compared with first line drugs such as pyrazinamide and were not cytotoxic in their respective MIC values. [Display omitted] A series of twenty-six pyrazine derivatives have been synthesized and evaluated against M. tuberculosis. Compounds 6, 23, 27 and 28 exhibited a significant activity (50–100 μg/mL).