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

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 h...

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Veröffentlicht in:Drug Discoveries & Therapeutics 2016, Vol.10(4), pp.188-194
Hauptverfasser: Panneerselvam, Theivendren, Sivakumar, Arumugam, Arumugam, Subramanian, Joshi, Shrinivas D.
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Sprache:eng
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Zusammenfassung: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.
ISSN:1881-7831
1881-784X
DOI:10.5582/ddt.2016.01048