Title: 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 #
Issue Date: Aug-2008
Publisher: Pergamon
Series Title: Bioorganic & Medicinal Chemistry vol:16 issue:15 pages:7429-35
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.
ISSN: 0968-0896
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Laboratory of Virology and Chemotherapy (Rega Institute)
× corresponding author
# (joint) last author

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