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通过结构修饰设计新的酰基硫代缩氨基脲的合成与抗结核活性。

Synthesis and antituberculosis activity of new acylthiosemicarbazides designed by structural modification.

机构信息

Universidad Nacional Autónoma de México, Instituto de Química, Ciudad Universitaria, Ciudad de México, México.

Instituto de Investigaciones Biomédicas, Universidad Nacional Autónoma de México, Ciudad Universitaria, Ciudad de México, México.

出版信息

Drug Dev Res. 2020 May;81(3):350-355. doi: 10.1002/ddr.21626. Epub 2019 Nov 28.

Abstract

Acylthiosemicarbazides 8a-n were designed by structural modification of lead Compound 7. The syntheses of 8a-n involve a five-step procedure starting from carboxylic acids. Compounds 8a-n were tested against three Mycobacterium tuberculosis strains to measure their inhibitory antituberculosis activities. These activities could be explained according to the presence or absence of the chlorine substituent in the aromatic ring of the amide joined to the thiosemicarbazide core. Thiosemicarbazide derivative 8n is a candidate for the development of novel antitubercular agents. Ongoing studies are focused on exploring the mechanism by which these compounds inhibit M. tuberculosis cell growth.

摘要

酰基硫代缩氨基脲 8a-n 是通过对先导化合物 7 进行结构修饰设计得到的。8a-n 的合成包括从羧酸开始的五步法。将化合物 8a-n 进行了抗三种结核分枝杆菌菌株的测试,以测量其抑制抗结核活性。根据酰胺连接到硫代缩氨基脲核心的芳环上有无氯取代基,可以解释这些活性。硫代缩氨基脲衍生物 8n 是开发新型抗结核药物的候选物。目前的研究集中在探索这些化合物抑制结核分枝杆菌细胞生长的机制。

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