Design, docking analysis, identification, and synthesis of novel 3-(((substituted phenyl) amino)methyl)-2-methylquinazolin-4(3H)-one compounds to fight tuberculosis.

doi:10.5582/ddt.2016.01048

Paper

Design, docking analysis, identification, and synthesis of novel 3-(((substituted phenyl) amino)methyl)-2-methylquinazolin-4(3H)-one compounds to fight tuberculosis.

Published 2016 · T. Panneerselvam, A. Sivakumar, S. Arumugam

Drug discoveries & therapeutics

Q2 SJR score

2

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0

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Abstract

In this study, a series of novel scaffold-based 3-(((substituted phenyl)amino)methyl)-2-methylquinazolin-4(3H)-one compounds, 3a-3r, was synthesized, characterized, and screened for its in vitro activity against the H37Ra strain of Mycobacterium tuberculosis. A number of analogs were found to have highly potent anti-tuberculosis activity. Compound 3m in particular had potent activity equal to that of the standard anti-tuberculosis drug rifampicin. New leads can be generated with the model developed in this study and this model will be optimized with the eventual goal of preparing new anti-tuberculosis agents.

In Vitro Study

Study Snapshot

Novel 3-(((substituted phenyl)amino)methyl)-2-methylquinazolin-4(3H)-one compounds show potent anti-tuberculosis activity, with compound 3m showing activity equal to rifampicin.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Design, docking analysis, identification, and synthesis of novel 3-(((substituted phenyl) amino)methyl)-2-methylquinazolin-4(3H)-one compounds to fight tuberculosis.

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