Novel N(1)-substituted 1,3-dihydro-2H-benzimidazol-2-ones as potent non-nucleoside reverse transcrip
July 3rd, 2008 | by admin |Novel N(1)-substituted 1,3-dihydro-2H-benzimidazol-2-ones as potent non-nucleoside reverse transcriptase inhibitors.
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.
Monforte AM, Rao A, Logoteta P, Ferro S, De Luca L, Barreca ML, Iraci N, Maga G, De Clercq E, Pannecouque C, Chimirri A.
Dipartimento Farmaco-Chimico, Università di Messina, Viale Annunziata, 98168 Messina, Italy.