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

Tonelli, Michele and Simone, Matteo and Tasso, Bruno and Novelli, Federica and Boido, Vito and Sparatore, Fabio and Paglietti, Giuseppe and Pricl, Sabrina and Giliberti, Gabriele and Blois, Sylvain and Ibba, Cristina and Sanna, Giuseppina and Loddo, Roberta and La Colla, Paolo (2010) Antiviral activity of benzimidazole derivatives. II. Antiviral activity of 2-phenylbenzimidazole derivatives. Bioorganic & Medicinal Chemistry, Vol. 18 (8), p. 2937-2953. eISSN 1464-3391. Article.

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DOI: 10.1016/j.bmc.2010.02.037


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.

Item Type:Article
ID Code:5637
Uncontrolled Keywords:2-Phenylbenzimidazole derivatives, antiviral activity, RNA and DNA viruses, NS5B RdRp inhibition
Subjects:Area 03 - Scienze chimiche > CHIM/08 Chimica farmaceutica
Divisions:001 Università di Sassari > 01 Dipartimenti > Farmaco, chimico, tossicologico
Publisher:Pergamon / Elsevier
Copyright Holders:© 2010 Elsevier
Deposited On:08 Mar 2011 14:09

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