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 (EC50 = 0.1–10 μM) against at least one virus, and four of them were outstanding for their high and selective activity against VV (24, EC50 = 0.1 μM) and BVDV (50, 51, and 53 with EC50 = 1.5, 0.8, and 1.0 μM, 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.

Antiviral activity of benzimidazole derivatives. II. Antiviral activity of 2-phenylbenzimidazole derivatives

GILIBERTI, GABRIELE;BLOIS, SYLVAIN SERGE DANIEL;IBBA, CRISTINA;SANNA, GIUSEPPINA;LODDO, ROBERTA;
2010

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 (EC50 = 0.1–10 μM) against at least one virus, and four of them were outstanding for their high and selective activity against VV (24, EC50 = 0.1 μM) and BVDV (50, 51, and 53 with EC50 = 1.5, 0.8, and 1.0 μM, 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.
2-Phenylbenzimidazole derivatives; Antiviral activity; NS5B RdRp inhibition; RNA and DNA viruses
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11584/94341
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