title: Antiviral activity of benzimidazole derivatives. II. Antiviral activity of 2-phenylbenzimidazole derivatives.
abstract: Seventy-six 2-phenylbenzimidazole derivatives were synthesized and evaluated in cell-based assays for cytotoxicity and antiviral activity against a panel of 10 RNA and DNA viruses. The most commonly affected viruses were, in decreasing order, CVB-2, BVDV, Sb-1, HSV-1, and YFV, while HIV-1 and VSV were not affected, and RSV, VV and Reo-1 were only susceptible to a few compounds. Thirty-nine compounds exhibited high activity (EC(50)=0.1-10microM) against at least one virus, and four of them were outstanding for their high and selective activity against VV (24, EC(50)=0.1microM) and BVDV (50, 51, and 53 with EC(50)=1.5, 0.8, and 1.0microM, respectively). The last compounds inhibited at low micromolar concentrations the NS5B RdRp of BVDV and also of HCV, the latter sharing structural similarity with the former. The considered compounds represent attractive leads for the development of antiviral agents against poxviruses, pestiviruses and even HCV, which are important human and veterinary pathogens.
authors.affiliation: Dipartimento di Scienze Farmaceutiche, Università di Genova, Viale Benedetto XV 3, 16132 Genova, Italy. michele.tonelli@unige.it
authors.forename: Michele
authors.initials: M
authors.lastname: Tonelli
authors.forename: Matteo
authors.initials: M
authors.lastname: Simone
authors.forename: Bruno
authors.initials: B
authors.lastname: Tasso
authors.forename: Federica
authors.initials: F
authors.lastname: Novelli
authors.forename: Vito
authors.initials: V
authors.lastname: Boido
authors.forename: Fabio
authors.initials: F
authors.lastname: Sparatore
authors.forename: Giuseppe
authors.initials: G
authors.lastname: Paglietti
authors.forename: Sabrina
authors.initials: S
authors.lastname: Pricl
authors.forename: Gabriele
authors.initials: G
authors.lastname: Giliberti
authors.forename: Sylvain
authors.initials: S
authors.lastname: Blois
authors.forename: Cristina
authors.initials: C
authors.lastname: Ibba
authors.forename: Giuseppina
authors.initials: G
authors.lastname: Sanna
authors.forename: Roberta
authors.initials: R
authors.lastname: Loddo
authors.forename: Paolo
authors.initials: P
authors.lastname: La Colla
mesh_terms: D000818:Animals; D000998:Antiviral Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D001562:Benzimidazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000633:toxicity; D002460:Cell Line; D002522:Chlorocebus aethiops; D006224:Cricetinae; D004267:DNA Viruses / Q000187:drug effects; D006801:Humans; D012328:RNA Viruses / Q000187:drug effects; D054852:Small Molecule Libraries; D013329:Structure-Activity Relationship; D014709:Vero Cells
chemical_list: D000998:Antiviral Agents; D001562:Benzimidazoles; D054852:Small Molecule Libraries; C117755:2-phenylbenzimidazole