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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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Detalles Bibliográficos
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
Descripción
Sumario: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.