One pot Click chemistry: A three component reaction for the synthesis of 2-mercaptobenzimidazole linked coumarinyl triazoles as anti-tubercular agents

被引：49

作者：

Anand, Ashish ^{[1
]}

Kulkarni, Manohar V. ^{[1
]}

Joshi, Shrinivas D. ^{[2
]}

Dixit, Sheshagiri R. ^{[2
]}

机构：

[1] Karnatak Univ, Dept Studies Chem, Dharwad 580003, Karnataka, India

[2] SETs Coll Pharm, Dept Pharmaceut Chem, Novel Drug Design & Discovery Lab, Dharwad 580002, Karnataka, India

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2016年 / 26卷 / 19期

关键词：

1,2,3-Triazoles; One pot Click reaction; 2H-Chromen-2-one; 2-Mercaptobenzimidazole; Anti-tubercular; Molecular docking; Surflex-Dock; MYCOBACTERIUM-TUBERCULOSIS; ANTITUBERCULAR ACTIVITY; LIGAND INTERACTIONS; SCORING FUNCTION; CYCLOADDITION; DPRE1; BENZOTHIAZINONES; DERIVATIVES; INHIBITION;

D O I：

10.1016/j.bmcl.2016.08.045

中图分类号：

R914 [药物化学];

学科分类号：

100705 [微生物与生化药学];

摘要：

2-Propargylthiobenzimidazole 1, 4-bromomethyl coumarins/1-aza-coumarins 2/3 and sodium azide have been reacted in one pot under Click chemistry conditions to give exclusively 1,4-disubstituted triazoles 5a-n. Anti-tubercular assays against M. tuberculosis (H(37)Rv) coupled with in silico molecular docking studies indicated that dimethyl substituents 5c and 5d showed promising activity with higher C-score values. (C) 2016 Elsevier Ltd. All rights reserved.

引用

页码：4709 / 4713

页数：5

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