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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...

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Autores principales: Nalla, Viswanadh, Shaikh, Aslam, Bapat, Sanket, Vyas, Renu, Karthikeyan, M., Yogeeswari, P., Sriram, D., Muthukrishnan, M.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: The Royal Society Publishing 2018
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.
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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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