Novel N1-substituted 1,3-dihydro-2H-benzimidazol-2-ones as potent non-nucleoside reverse transcriptase inhibitors |
| |
Authors: | Monforte Anna-Maria Rao Angela Logoteta Patrizia Ferro Stefania De Luca Laura Barreca Maria Letizia Iraci Nunzio Maga Giovanni De Clercq Erik Pannecouque Christophe Chimirri Alba |
| |
Affiliation: | Dipartimento Farmaco-Chimico, Università di Messina, Viale Annunziata, 98168 Messina, Italy. ammonforte@pharma.unime.it |
| |
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. |
| |
Keywords: | |
本文献已被 PubMed 等数据库收录! |
|