Dimers of coumarin-1,2,3-triazole hybrids bearing alkyl spacer: Design, microwave-assisted synthesis, molecular docking and evaluation as antimycobacterial and antimicrobial agents

被引：51

作者：

Ashok, Dongamanti ^{[1
]}

Gundu, Srinivas ^{[1
]}

Aamate, Vikas Kumar ^{[1
]}

Devulapally, Mohan Gandhi ^{[1
]}

Bathini, Raju ^{[2
]}

Manga, Vijjulatha ^{[2
]}

机构：

[1] Osmania Univ, Green & Med Chem Lab, Dept Chem, Hyderabad 500007, Telangana, India

[2] Osmania Univ, Dept Chem, Mol Modeling & Med Chem Lab, Hyderabad 500007, Telangana, India

来源：

JOURNAL OF MOLECULAR STRUCTURE | 2018年 / 1157卷

关键词：

Coumarin; 1,2,3-Triazole; Cycloaddition; Antimicrobial; Antimycobacterial; Molecular docking; TUBERCULOSIS PANTOTHENATE SYNTHETASE; MYCOBACTERIUM-TUBERCULOSIS; DRUG DISCOVERY; COUMARIN DERIVATIVES; HIV-1; PROTEASE; INHIBITORS; ANTIOXIDANT; 1,2,3-TRIAZOLES; TRIAZOLES; ASSAY;

D O I：

10.1016/j.molstruc.2017.12.080

中图分类号：

O64 [物理化学（理论化学）、化学物理学];

学科分类号：

070304 ; 081704 ;

摘要：

The present study demonstrated the synthesis of new series of coumarin-1,2,3-triazole hybrids under microwave irradiation method. Several dimers of coumarin based 1,2,3-triazole derivatives were synthesized and their antimycobacterial and antimicrobial activities were investigated. The antimycobacterial activity screening results revealed that compounds 6i and 6j were the most active against Mycobacterium tuberculosis H37Rv strain. The active compounds were further evaluated for cytotoxicity with HEK cell lines and exhibited less % of inhibition. The same synthetic hybrids were evaluated for their antimicrobial activity against various bacterial strains and fungal strains and compounds 6e, 6h, 6i and 6j were found to be the most promising antimicrobial potent molecules. Furthermore, the active compounds against Mycobacterium tuberculosis were evaluated for their molecular docking studies against pantothenate synthetase (PS) enzyme of MTB and the docking results are in well agreement with the antitubercular evaluation results. (C) 2017 Elsevier B.V. All rights reserved.

引用

页码：312 / 321

页数：10

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