2. Academic Validation
  3. Novel N1-substituted 1,3-dihydro-2H-benzimidazol-2-ones as potent non-nucleoside reverse transcriptase inhibitors

Novel N1-substituted 1,3-dihydro-2H-benzimidazol-2-ones as potent non-nucleoside reverse transcriptase inhibitors

  • Bioorg Med Chem. 2008 Aug 1;16(15):7429-35. doi: 10.1016/j.bmc.2008.06.012.
Anna-Maria Monforte 1,  Angela Rao,  Patrizia Logoteta,  Stefania Ferro,  Laura De Luca,  Maria Letizia Barreca,  Nunzio Iraci,  Giovanni Maga,  Erik De Clercq,  Christophe Pannecouque,  Alba Chimirri
Affiliations

Affiliation

  • 1 Dipartimento Farmaco-Chimico, Università di Messina, Viale Annunziata, 98168 Messina, Italy. ammonforte@pharma.unime.it
PMID: 18585918 DOI: 10.1016/j.bmc.2008.06.012
Abstract

Several N(1)-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 N(1) and on the benzene ring of benzimidazolone moiety significantly influenced the anti-HIV activity of this class of potent antiretroviral agents.

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