新型 L-丝氨酰腙衍生物的合成及抗结核活性。
Synthesis and antitubercular activity of new L-serinyl hydrazone derivatives.
机构信息
Fundação Oswaldo Cruz, Instituto de Tecnologia em Fármacos-Far Manguinhos, Fundação Oswaldo Cruz, 21041-250, Rio de Janeiro, RJ, Brazil.
出版信息
Med Chem. 2011 Nov;7(6):611-23. doi: 10.2174/157340611797928325.
A series of 32 L-serinyl hydrazone derivatives have been synthesized and evaluated for their in vitro antibacterial activity against Mycobacterium tuberculosis H37Rv, being also evaluated their cell viabilities in non infected and infected macrophages with Mycobacterium bovis Bacillus Calmette-Guerin (BCG). The compounds 8c, 8e, 8h and 8i, were non-cytotoxic and exhibited an important minimum inhibitory concentration (MIC) activity between 25 and 100 μg/mL, which can be compared with that of the tuberculostatic drug D-cicloserine (5-20 μg/mL).
已经合成了一系列 32 种 L-丝氨酰腙衍生物，并评估了它们对结核分枝杆菌 H37Rv 的体外抗菌活性，同时还评估了它们在未感染和感染牛分枝杆菌卡介苗（BCG）的巨噬细胞中的细胞活力。化合物 8c、8e、8h 和 8i 无细胞毒性，并且在 25 至 100 μg/mL 之间表现出重要的最小抑菌浓度（MIC）活性，可与抗结核药物 D-环丝氨酸（5-20 μg/mL）相媲美。
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