title: 5-acetyl-2-arylbenzimidazoles as antiviral agents. Part 4.
abstract: Within a project aimed at discovering new Flaviviridae inhibitors, new variously substituted 2-phenylbenzimidazoles were synthesized and evaluated in cell-based assays for cytotoxicity and antiviral activity against viruses representatives of the three genera of the Flaviviridae family, i.e.: Pestivirus (BVDV), Flavivirus (YFV) and Hepacivirus (HCV). Title compounds were also tested against RNA viruses representative of other single-stranded, positive-sense (ssRNA(+)) negative-sense (RNA(-)), or double-stranded (dsRNA) genomes, as well as against representatives of two DNA virus families. Nine compounds showed activity against BVDV (EC(50) = 0.8-8.0 μM), compound 31 being the most potent (EC(50) = 0.80 μM) and selective (SI = CC(50)/EC(50) = >100). When tested in an HCV replicon assay, compound 31 resulted again the most potent, displaying an EC(50) value of 1.11 μM and an SI of 100. Besides inhibiting BVDV, two compounds (35 and 38) showed a moderate activity also against YFV (EC(50) = 13 μM). Interestingly, 35 was moderately active also against RSV (EC(50) = 25 μM).
authors.affiliation: Dipartimento di Scienza del Farmaco, Università degli Studi di Sassari, Via Muroni 23/a, 07100 Sassari, Italy.
authors.forename: Gabriella
authors.initials: G
authors.lastname: Vitale
authors.forename: Paola
authors.initials: P
authors.lastname: Corona
authors.forename: Mario
authors.initials: M
authors.lastname: Loriga
authors.forename: Antonio
authors.initials: A
authors.lastname: Carta
authors.forename: Giuseppe
authors.initials: G
authors.lastname: Paglietti
authors.forename: Gabriele
authors.initials: G
authors.lastname: Giliberti
authors.forename: Giuseppina
authors.initials: G
authors.lastname: Sanna
authors.forename: Pamela
authors.initials: P
authors.lastname: Farci
authors.forename: Maria Elena
authors.initials: ME
authors.lastname: Marongiu
authors.forename: Paolo
authors.initials: P
authors.lastname: La Colla
mesh_terms: D000818:Animals; D000998:Antiviral Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology* / Q000633:toxicity; D001562:Benzimidazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology* / Q000633:toxicity; D002417:Cattle; D002460:Cell Line; D006224:Cricetinae; D015195:Drug Design; D014780:Viruses / Q000187:drug effects*
chemical_list: D000998:Antiviral Agents; D001562:Benzimidazoles