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Identification of potent chromone embedded [1,2,3]-triazoles as novel anti-tubercular agents
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 inhib...
Autores principales: | , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
The Royal Society Publishing
2018
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5936909/ https://www.ncbi.nlm.nih.gov/pubmed/29765644 http://dx.doi.org/10.1098/rsos.171750 |
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author | Nalla, Viswanadh Shaikh, Aslam Bapat, Sanket Vyas, Renu Karthikeyan, M. Yogeeswari, P. Sriram, D. Muthukrishnan, M. |
author_facet | Nalla, Viswanadh Shaikh, Aslam Bapat, Sanket Vyas, Renu Karthikeyan, M. Yogeeswari, P. Sriram, D. Muthukrishnan, M. |
author_sort | Nalla, Viswanadh |
collection | PubMed |
description | 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. |
format | Online Article Text |
id | pubmed-5936909 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2018 |
publisher | The Royal Society Publishing |
record_format | MEDLINE/PubMed |
spelling | pubmed-59369092018-05-15 Identification of potent chromone embedded [1,2,3]-triazoles as novel anti-tubercular agents Nalla, Viswanadh Shaikh, Aslam Bapat, Sanket Vyas, Renu Karthikeyan, M. Yogeeswari, P. Sriram, D. Muthukrishnan, M. R Soc Open Sci Chemistry 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. The Royal Society Publishing 2018-04-04 /pmc/articles/PMC5936909/ /pubmed/29765644 http://dx.doi.org/10.1098/rsos.171750 Text en © 2018 The Authors. http://creativecommons.org/licenses/by/4.0/ Published by the Royal Society under the terms of the Creative Commons Attribution License http://creativecommons.org/licenses/by/4.0/, which permits unrestricted use, provided the original author and source are credited. |
spellingShingle | Chemistry Nalla, Viswanadh Shaikh, Aslam Bapat, Sanket Vyas, Renu Karthikeyan, M. Yogeeswari, P. Sriram, D. Muthukrishnan, M. Identification of potent chromone embedded [1,2,3]-triazoles as novel anti-tubercular agents |
title | Identification of potent chromone embedded [1,2,3]-triazoles as novel anti-tubercular agents |
title_full | Identification of potent chromone embedded [1,2,3]-triazoles as novel anti-tubercular agents |
title_fullStr | Identification of potent chromone embedded [1,2,3]-triazoles as novel anti-tubercular agents |
title_full_unstemmed | Identification of potent chromone embedded [1,2,3]-triazoles as novel anti-tubercular agents |
title_short | Identification of potent chromone embedded [1,2,3]-triazoles as novel anti-tubercular agents |
title_sort | identification of potent chromone embedded [1,2,3]-triazoles as novel anti-tubercular agents |
topic | Chemistry |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5936909/ https://www.ncbi.nlm.nih.gov/pubmed/29765644 http://dx.doi.org/10.1098/rsos.171750 |
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