title: Synthesis and antimycobacterial activity of N'-[(E)-(monosubstituted-benzylidene)]-2-pyrazinecarbohydrazide derivatives.
abstract: 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.
authors.affiliation: Fundação Oswaldo Cruz, Instituto de Tecnologia em Fármacos-Far Manguinhos, Fundação Oswaldo Cruz, 21041-250, Rio de Janeiro, RJ, Brazil.
authors.forename: Fátima M F
authors.initials: FM
authors.lastname: Vergara
authors.forename: Camilo H da S
authors.initials: CH
authors.lastname: Lima
authors.forename: Maria das Graças M de O
authors.initials: Md
authors.lastname: Henriques
authors.forename: André L P
authors.initials: AL
authors.lastname: Candéa
authors.forename: Maria C S
authors.initials: MC
authors.lastname: Lourenço
authors.forename: Marcelle de L
authors.initials: Mde L
authors.lastname: Ferreira
authors.forename: Carlos R
authors.initials: CR
authors.lastname: Kaiser
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 / Q000494:pharmacology; D001597:Benzylidene Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002470:Cell Survival; D015195:Drug Design; D006801:Humans; D006834:Hydrazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D008264:Macrophages / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D011718:Pyrazinamide / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000900:Anti-Bacterial Agents; D000995:Antitubercular Agents; D001597:Benzylidene Compounds; D006834:Hydrazines; D011718:Pyrazinamide; C019289:carbohydrazide