Oxazolone-1,2,3-Triazole Hybrids: Design, Synthesis and Antimicrobial Evaluation

被引：20

作者：

Lal, Kashmiri ^{[1
]}

Kumar, Lokesh ^{[1
]}

Kumar, Ashwani ^{[2
]}

Kumar, Anil ^{[3
]}

机构：

[1] Guru Jambheshwar Univ Sci & Technol, Dept Chem, Hisar 125001, Haryana, India

[2] Guru Jambheshwar Univ Sci & Technol, Dept Pharmaceut Sci, Hisar 125001, Haryana, India

[3] Guru Jambheshwar Univ Sci & Technol, Dept Bio & Nanotechnol, Hisar 125001, Haryana, India

来源：

CURRENT TOPICS IN MEDICINAL CHEMISTRY | 2018年 / 18卷 / 17期

关键词：

1,2,3-Triazoles; Click Chemistry; Oxazolones; Antimicrobial activity; Docking studies; Hybrids; BIOLOGICAL EVALUATION; CLICK CHEMISTRY; DERIVATIVES; INHIBITORS; DOCKING;

D O I：

10.2174/1568026618666180913110456

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Background: Oxazolones and 1,2,3-triazoles are among the extensively studied heterocycles in medicinal chemistry. Both of these moieties are reported to possess a broad spectrum of biological activity including antimicrobial. Objective: The objective of the current work is to design, synthesize and antimicrobial evaluation of some new oxazolone-1,2,3-triazole hybrids. Methods: The designed oxazolone-1,2,3-triazole hybrids were synthesized using copper(I)-catalyzed azide-alkyne cycloaddition. The antimicrobial evaluation was carried out using serial dilution method. Results: Most of the synthesized hybrids showed significant antimicrobial properties. Some of the compounds were found to be possessing better or comparable activity to that of the standards used. The docking simulations results are also in agreement with the antimicrobial activity data. Conclusion: Sixteen new hybrids were synthesized and tested in vitro for their antimicrobial activity. Some of the tested compounds exhibited promising antimicrobial activity and could be utilized for the development of the lead compounds for new and more potent antimicrobial drugs.

引用

页码：1506 / 1513

页数：8

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