Drug Discov Ther. 2016;10(4):188-194. (DOI: 10.5582/ddt.2016.01048)

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

Panneerselvam T, Sivakumar A, Arumugam S, Shrinivas D Joshi


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.

KEYWORDS: Quinazoline, amines, antimicrobial activity, antituberculosis activity

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