title: Novel N1-substituted 1,3-dihydro-2H-benzimidazol-2-ones as potent non-nucleoside reverse transcriptase inhibitors.
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.
authors.affiliation: Dipartimento Farmaco-Chimico, Università di Messina, Viale Annunziata, 98168 Messina, Italy. ammonforte@pharma.unime.it
authors.forename: Anna-Maria
authors.initials: AM
authors.lastname: Monforte
authors.forename: Angela
authors.initials: A
authors.lastname: Rao
authors.forename: Patrizia
authors.initials: P
authors.lastname: Logoteta
authors.forename: Stefania
authors.initials: S
authors.lastname: Ferro
authors.forename: Laura
authors.initials: L
authors.lastname: De Luca
authors.forename: Maria Letizia
authors.initials: ML
authors.lastname: Barreca
authors.forename: Nunzio
authors.initials: N
authors.lastname: Iraci
authors.forename: Giovanni
authors.initials: G
authors.lastname: Maga
authors.forename: Erik
authors.initials: E
authors.lastname: De Clercq
authors.forename: Christophe
authors.initials: C
authors.lastname: Pannecouque
authors.forename: Alba
authors.initials: A
authors.lastname: Chimirri
mesh_terms: D019380:Anti-HIV Agents / Q000737:chemistry / Q000494:pharmacology; D001562:Benzimidazoles / Q000737:chemistry* / Q000494:pharmacology*; D002460:Cell Line; D015497:HIV-1 / Q000187:drug effects; D006801:Humans; D008958:Models, Molecular; D015394:Molecular Structure; D018894:Reverse Transcriptase Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014779:Virus Replication
chemical_list: D019380:Anti-HIV Agents; D001562:Benzimidazoles; D018894:Reverse Transcriptase Inhibitors