title: Design, synthesis, and structure-activity relationships of 1,3-dihydrobenzimidazol-2-one analogues as anti-HIV agents.
abstract: Non-nucleoside reverse transcriptase inhibitors (NNRTIs) have become very important components in the antiretroviral combination therapies used to treat HIV. Recently, our group identified some 1,3-dihydrobenzimidazol-2-one derivatives and their sulfones as a potent and novel class of NNRTIs. We herein report the synthesis and biological evaluation of the new compounds in which different structural modifications have been introduced in order to investigate their effects on RT inhibition.
authors.affiliation: Dipartimento Farmaco-Chimico, Università di Messina, Italy. ammonforte@pharma.unime.it
authors.forename: Anna-Maria
authors.initials: AM
authors.lastname: Monforte
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: Nunzio
authors.initials: N
authors.lastname: Iraci
authors.forename: Giovanni
authors.initials: G
authors.lastname: Maga
authors.forename: Erik De
authors.initials: ED
authors.lastname: 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 / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001562:Benzimidazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D002460:Cell Line; D015195:Drug Design; D054303:HIV Reverse Transcriptase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D006801:Humans; D018894:Reverse Transcriptase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D019380:Anti-HIV Agents; D001562:Benzimidazoles; D018894:Reverse Transcriptase Inhibitors; C014353:benzimidazolone; D054303:HIV Reverse Transcriptase