title: Synthesis and antimycobacterial evaluation of N'-(E)-heteroaromaticpyrazine-2-carbohydrazide derivatives.
abstract: A series of nine N'-(E)-heteroaromatic-pyrazine-2-carbohydrazide derivatives (5a-f and 6a-c) have been synthesized and evaluated against M. tuberculosis ATCC 27294 using the micro plate Alamar Blue assay (MABA), being the activities expressed as the minimum inhibitory concentration (MIC) in µg/ml. Compounds 5a and 5f exhibited potent activities (3.12 and 50µg/mL, respectively) when compared to the first line drug pyrazinamide (MIC>100 µg/mL). Afterwards, these compounds were evaluated for their cell viabilities in non-infected and infected macrophages with Mycobaterium bovis Bacillus Calmette-Guerin (BCG) and 5f was not cytotoxic to host cells in the effective concentration to inhibit the growth of M. tuberculosis.
authors.affiliation: Fundação Oswaldo Cruz, Instituto de Tecnologia em Fármacos-Far Manguinhos, Fundação Oswaldo Cruz, Rio de Janeiro, RJ, Brazil.
authors.forename: C H S
authors.initials: CH
authors.lastname: Lima
authors.forename: M G M O
authors.initials: MG
authors.lastname: Henriques
authors.forename: A L P
authors.initials: AL
authors.lastname: Candéa
authors.forename: M C S
authors.initials: MC
authors.lastname: Lourenço
authors.forename: F A F M
authors.initials: FA
authors.lastname: Bezerra
authors.forename: M L
authors.initials: ML
authors.lastname: Ferreira
authors.forename: C R
authors.initials: CR
authors.lastname: Kaiser
authors.forename: M V N
authors.initials: MV
authors.lastname: de Souza
mesh_terms: D000818:Animals; D000995:Antitubercular Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D006834:Hydrazines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D008264:Macrophages / Q000187:drug effects; D051379:Mice; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D011719:Pyrazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013237:Stereoisomerism
chemical_list: D000995:Antitubercular Agents; D006834:Hydrazines; D011719:Pyrazines; C019289:carbohydrazide