Identification of potent chromone embedded [1,2,3]-triazoles as novel anti-tubercular agents

Author:

Nalla Viswanadh12,Shaikh Aslam12,Bapat Sanket3,Vyas Renu3,Karthikeyan M.12,Yogeeswari P.4,Sriram D.4,Muthukrishnan M.12ORCID

Affiliation:

1. CSIR-National Chemical Laboratory, Dr Homi Bhabha Road, Pune 411008, India

2. Academy of Scientific and Innovative Research (AcSIR), New Delhi 110 025, India

3. MIT School of Bioengineering Sciences and Research, MIT Art, Design and Technology University, Pune 412 201, India

4. Tuberculosis Drug Discovery Laboratory, Pharmacy Group, Birla Institute of Technology and Science-Pilani, Hyderabad Campus, Hyderabad 500 0078, India

Abstract

A series of 20 novel chromone embedded [1,2,3]-triazoles derivatives were synthesized via an easy and convenient synthetic procedure starting from 2-hydroxy acetophenone. The in vitro anti-mycobacterial evaluation studies carried out in this work reveal that seven compounds exhibit significant inhibition against Mycobacterium tuberculosis H37Rv strain with MIC in the range of 1.56–12.5 µg ml −1 . Noticeably, compound 6s was the most potent compound in vitro with a MIC value of 1.56 µg ml −1 . Molecular docking and chemoinformatics studies revealed that compound 6s displayed drug-like properties against the enoyl-acyl carrier protein reductase of M. tuberculosis further establishing its potential as a potent inhibitor.

Publisher

The Royal Society

Subject

Multidisciplinary

Reference37 articles.

1. World Health Organization Global Tuberculosis Report 2016 (http://www.who.int/tb/publications/global_report/en/)

2. Exploiting the synthetic lethality between terminal respiratory oxidases to kill Mycobacterium tuberculosis and clear host infection

3. The Growing Burden of Tuberculosis

4. Drug-resistant tuberculosis;Long R;CMAJ,2000

5. HIV-associated tuberculosis in the era of HAART;Pozniak A;Int. J. Tuberc. Lung Dis.,2000

同舟云学术

1.学者识别学者识别

2.学术分析学术分析

3.人才评估人才评估

"同舟云学术"是以全球学者为主线,采集、加工和组织学术论文而形成的新型学术文献查询和分析系统,可以对全球学者进行文献检索和人才价值评估。用户可以通过关注某些学科领域的顶尖人物而持续追踪该领域的学科进展和研究前沿。经过近期的数据扩容,当前同舟云学术共收录了国内外主流学术期刊6万余种,收集的期刊论文及会议论文总量共计约1.5亿篇,并以每天添加12000余篇中外论文的速度递增。我们也可以为用户提供个性化、定制化的学者数据。欢迎来电咨询!咨询电话:010-8811{复制后删除}0370

www.globalauthorid.com

TOP

Copyright © 2019-2024 北京同舟云网络信息技术有限公司
京公网安备11010802033243号  京ICP备18003416号-3