Title: Novel 1,3-dihydro-benzimidazol-2-ones and their analogues as potent non-nucleoside HIV-1 reverse transcriptase inhibitors
Authors: Monforte, AM
Logoteta, P
Luca, LD
Iraci, N
Ferro, S
Maga, G
De Clercq, Erik
Pannecouque, Christophe ×
Chimirri, A #
Issue Date: Feb-2010
Publisher: Pergamon
Series Title: Bioorganic & Medicinal Chemistry vol:18 issue:4 pages:1702-1710
Abstract: A series of novel benzimidazolones and their analogues, characterized by the presence of one or more
methyl groups or other bioisosteric moieties at different positions of the phenyl ring at N-1, were synthesized
and evaluated as inhibitors of human immunodeficiency virus type-1 (HIV-1). Most of the new
compounds proved to be highly effective in inhibiting both HIV-1 replication in MT4 cells with minimal
cytotoxicity and RT enzyme at nanomolar concentrations. Some derivatives were also tested against RTs
containing single amino acid mutations responsible for resistance to non-nucleoside reverse transcriptase
inhibitors (NNRTIs). The different potencies displayed by the new compounds were studied using
molecular modeling.
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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