Title of article
Novel N1-substituted 1,3-dihydro-2H-benzimidazol-2-ones as potent non-nucleoside reverse transcriptase inhibitors Original Research Article
Author/Authors
Anna-Maria Monforte، نويسنده , , Angela Rao، نويسنده , , Patrizia Logoteta، نويسنده , , Stefania Ferro، نويسنده , , Laura De Luca، نويسنده , , Maria Letizia Barreca، نويسنده , , Nunzio Iraci، نويسنده , , Giovanni Maga، نويسنده , , Erik De Clercq، نويسنده , , Christophe Pannecouque، نويسنده , , Alba Chimirri، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
7
From page
7429
To page
7435
Abstract
Several N1-substituted 1,3-dihydro-2H-benzimidazol-2-ones were synthesized and evaluated as anti-HIV agents. Some of them proved to be highly effective in inhibiting HIV-1 replication at nanomolar concentration as potent non-nucleoside HIV-1 RT inhibitors (NNRTIs) with low cytotoxicity. SAR studies highlighted that the nature of the substituents at N1 and on the benzene ring of benzimidazolone moiety significantly influenced the anti-HIV activity of this class of potent antiretroviral agents.
Keywords
RT inhibitors , Benzimidazolones , Molecular modeling , Microwave-assisted synthesis
Journal title
Bioorganic and Medicinal Chemistry
Serial Year
2008
Journal title
Bioorganic and Medicinal Chemistry
Record number
1306792
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