Antitubercular activity of 1,2,3-triazolyl fatty acid derivatives
Antitubercular activity of 1,2,3-triazolyl fatty acid derivatives
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DOI：
10.1016/j.ejmech.2016.09.086
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发表时间：
2017-01-05
影响因子：
6.7
通讯作者：
Labadie, Guillermo R.
中科院分区：
文献类型：
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作者：
Ghiano, Diego G.;de la Iglesia, Agustina;Labadie, Guillermo R.
利用点击化学法合成了一系列1，2，3-三唑类不饱和脂肪酸模拟物。制备的1，4-二取代类似物覆盖不同的烷基链长度和三唑位置。随后测试了化合物对结核分枝杆菌的作用，其中大多数化合物具有活性，一些类似物在微摩尔浓度下显示活性。该系列中最有效的成员在C-2位上具有三唑部分，其碳链具有8个或10个碳原子。最具活性的类似物的1，5-异构体的活性显著低于原始异构体。在提供相同MIC的几种临床MTB多药耐药菌株上测定所选命中物的活性。(C)2016 Elsevier Masson SAS。All rights reserved.
A collection of 1,2,3-triazoles unsaturated fatty acid mimics were efficiently synthesized by click chemistry. The 1,4-disubstituted analogs prepared covered different alkyl chain lengths and triazole positions. The compounds were subsequently tested against Mycobacterium tuberculosis, being most of them active with some of the analogs displaying activity at micromolar concentration. The most potent member of the series has the triazole moiety on the C-2 position with a carbon chain of eight or ten carbon atoms. The 1,5-isomers of the most active analog were significantly less active than the original isomer. The activity of the selected hit was assayed on several clinical MTB multi-drug resistant strains providing the same MIC. (C) 2016 Elsevier Masson SAS. All rights reserved.