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5-Acetyl-2-arylbenzimidazoles as antiviral agents: part 4

Vitale, Gabriella and Corona, Paola and Loriga, Mario and Carta, Antonio and Paglietti, Giuseppe and Giliberti, Gabriele and Sanna, Giuseppina and Farci, Pamela and Marongiu, Maria Elena and La Colla, Paolo (2012) 5-Acetyl-2-arylbenzimidazoles as antiviral agents: part 4. European Journal of Medicinal Chemistry, Vol. 53 , p. 83-97. eISSN 1768-3254. Article.

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DOI: 10.1016/j.ejmech.2012.03.038

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 (EC50 = 0.8–8.0 μM), compound 31 being the most potent (EC50 = 0.80 μM) and selective (SI = CC50/EC50 = >100). When tested in an HCV replicon assay, compound 31 resulted again the most potent, displaying an EC50 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 (EC50 = 13 μM). Interestingly, 35 was moderately active also against RSV (EC50 = 25 μM).

Item Type:Article
ID Code:8571
Status:Published
Refereed:Yes
Uncontrolled Keywords:5-acetyl-2-arylbenzimidazoles, semi and thiosemicarbazones, ketoximes, antiflaviviridae virus activity
Subjects:Area 03 - Scienze chimiche > CHIM/08 Chimica farmaceutica
Divisions:001 Università di Sassari > 01-a Nuovi Dipartimenti dal 2012 > Chimica e Farmacia
Publisher:Elsevier
eISSN:1768-3254
Deposited On:30 Jan 2013 16:31

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