N'-(E)-杂环吡嗪-2-甲酰肼衍生物的合成及抗分枝杆菌活性评价。
Synthesis and antimycobacterial evaluation of N'-(E)-heteroaromaticpyrazine-2-carbohydrazide derivatives.
机构信息
Fundação Oswaldo Cruz, Instituto de Tecnologia em Fármacos-Far Manguinhos, Fundação Oswaldo Cruz, Rio de Janeiro, RJ, Brazil.
出版信息
Med Chem. 2011 May;7(3):245-9. doi: 10.2174/157340611795564303.
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.
已经合成了一系列九个 N'-(E)-杂芳基吡嗪-2-甲酰肼衍生物（5a-f 和 6a-c），并使用微量板 Alamar Blue 测定法（MABA）对结核分枝杆菌 ATCC 27294 进行了评估，其活性以最小抑制浓度（MIC）表示（以 µg/ml 计）。与一线药物吡嗪酰胺（MIC>100 µg/ml）相比，化合物 5a 和 5f 表现出很强的活性（分别为 3.12 和 50µg/mL）。随后，在未感染和感染有牛分枝杆菌卡介苗（BCG）的巨噬细胞中评估了这些化合物的细胞活力，而 5f 在有效浓度下对宿主细胞没有细胞毒性，能够抑制结核分枝杆菌的生长。
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