title: Synthesis and anti-hIV activity of 1-(2,6-difluorophenyl)-1H,3H-thiazolo[3,4-a]benzimidazole structurally-related 1,2-substituted benzimidazoles.
abstract: The synthesis of 1,2-substituted benzimidazoles is reported. These novel derivatives share chemical similarities with 1-aryl-1H,3H-thiazolo[3,4-a]benzimidazoles, a class of HIV-1 NNRTIs studied widely. All compounds prepared were tested in MT-4 cells to explore their potential anti-HIV activity and were found to be less potent than 1-(2,6-difluorophenyl)-1H,3H-thiazolo[3,4-a]benzimidazole (TBZ).
authors.affiliation: Dipartimento Farmaco-Chimico, Università di Messina, Italy. a.rao@pharma.unime.it
authors.forename: Angela
authors.initials: A
authors.lastname: Rao
authors.forename: Alba
authors.initials: A
authors.lastname: Chimirri
authors.forename: Erik
authors.initials: E
authors.lastname: De Clercq
authors.forename: Anna Maria
authors.initials: AM
authors.lastname: Monforte
authors.forename: Pietro
authors.initials: P
authors.lastname: Monforte
authors.forename: Christophe
authors.initials: C
authors.lastname: Pannecouque
authors.forename: Maria
authors.initials: M
authors.lastname: Zappalà
mesh_terms: D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D001562:Benzimidazoles / Q000737:chemistry* / Q000494:pharmacology*; D002461:Cell Line, Transformed; D015497:HIV-1 / Q000187:drug effects; D015498:HIV-2 / Q000187:drug effects; D006801:Humans; D007928:Lethal Dose 50; D008958:Models, Molecular; D018894:Reverse Transcriptase Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014779:Virus Replication / Q000187:drug effects
chemical_list: D019380:Anti-HIV Agents; D001562:Benzimidazoles; D018894:Reverse Transcriptase Inhibitors