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新型氨基酸衍生物的合成及抗结核活性。

Synthesis and antitubercular activity of novel amino acid derivatives.

机构信息

Instituto de Tecnologia em Fármacos - Farmanguinhos, FioCruz - Fundação Oswaldo Cruz, R. Sizenando Nabuco, 100 Manguinhos, 21041-250 Rio de Janeiro, RJ, Brazil.

出版信息

Chem Biol Drug Des. 2012 Feb;79(2):216-22. doi: 10.1111/j.1747-0285.2011.01269.x. Epub 2012 Jan 4.

Abstract

In this work, 17 new N-acylhydrazone derivatives of amino acids have been evaluated for their in vitro antibacterial activity against Mycobacterium tuberculosis H37Rv. The compounds 8b, 8e, 8f, 9a-d, and 10c exhibited an important minimum inhibitory concentration activity between 12.5 and 50 μg/mL, which can be compared with that of the tuberculostatic drug d-cycloserine (20 μg/mL).

摘要

在这项工作中,评估了 17 种新的氨基酸 N-酰腙衍生物对结核分枝杆菌 H37Rv 的体外抗菌活性。化合物 8b、8e、8f、9a-d 和 10c 的最小抑菌浓度活性在 12.5 至 50μg/mL 之间,可与分枝杆菌抑制药物 D-环丝氨酸(20μg/mL)相媲美。

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