Identification of potent chromone embedded [1,2,3]-triazoles as novel anti-tubercular agents
Author(s) -
Viswanadh Nalla,
Aslam C. Shaikh,
Sanket Bapat,
Renu Vyas,
Muthukumarasamy Karthikeyan,
Perumal Yogeeswari,
Dharmarajan Sriram,
M. Muthukrishnan
Publication year - 2018
Publication title -
royal society open science
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.84
H-Index - 51
ISSN - 2054-5703
DOI - 10.1098/rsos.171750
Subject(s) - chromone , mycobacterium tuberculosis , acetophenone , cheminformatics , chemistry , docking (animal) , in vitro , stereochemistry , inha , combinatorial chemistry , tuberculosis , biochemistry , medicine , computational chemistry , catalysis , nursing , pathology
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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