Synthesis and biological evaluation of novel 1,2,3-triazole derivatives as anti-tubercular agents

被引：78

作者：

Ali, Abdul Aziz ^{[1
]}

Gogoi, Dhrubajyoti ^{[2
]}

Chaliha, Amrita K. ^{[2
]}

Buragohain, Alak K. ^{[2
]}

Trivedi, Priyanka ^{[3
]}

Saikia, Prakash J. ^{[4
]}

Gehlot, Praveen S. ^{[5
]}

Kumar, Arvind ^{[5
]}

Chaturvedi, Vinita ^{[3
]}

Sarma, Diganta ^{[1
]}

机构：

[1] Dibrugarh Univ, Dept Chem, Dibrugarh 786004, Assam, India

[2] Dibrugarh Univ, Ctr Biotechnol & Bioinformat, DBT Bioinformat Infrastruct Facil, Dibrugarh 786004, Assam, India

[3] CSIR, Cent Drug Res Inst, Biochem Div, Lucknow 226001, Uttar Pradesh, India

[4] CSIR North East Inst Sci & Technol, Analyt Chem Div, Jorhat 785006, Assam, India

[5] CSIR Cent Salt & Marine Chem Res Inst, Salt & Marine Chem Div, AcSIR, Bhavnagar 364002, Gujarat, India

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2017年 / 27卷 / 16期

关键词：

Tuberculosis; 1,2,3-Triazoles; Antimycobacterial activity; Cytotoxicity; Molecular docking; ALKYNE CYCLOADDITION REACTIONS; INHIBITORS; DESIGN; ANTICANCER; TRIAZOLES;

D O I：

10.1016/j.bmcl.2017.07.008

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A library of seventeen novel 1,2,3-triazole derivatives were efficiently synthesized in excellent yields by the popular 'click chemistry' approach and evaluated in vitro for their anti-tubercular activity against Mycobacterium tuberculosis H37Ra (ATCC 25177 strain). Among the series, six compounds exhibited significant activity with minimum inhibitory concentration (MIC) values ranging from 3.12 to 0.78 mu g/mL and along with no significant cytotoxicity against MBMDMQs (mouse bone marrow derived macrophages). Molecular docking of the target compounds into the active site of DprEl (Decaprenylphosphoryl-beta-D-ribose-2'-epimerase) enzyme revealed noteworthy information on the plausible binding interactions. (C) 2017 Elsevier Ltd. All rights reserved.

引用

页码：3698 / 3703

页数：6

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