A library of eighty-six assorted benzimidazole derivatives was screened for antiviral activity against a panel of ten RNA and DNA viruses. Fifty-two of them displayed different levels of activity against one or more viruses, among which CVB-5, RSV, BVDV and Sb-1 were the most frequently affected. In particular, fourteen compounds exhibited an EC50 in the range 9-17 μM (SI from 6 to >11) versus CVB-5, and seven compounds showed an EC50 in the range 5-15 μM (SI from 6.7 to ≥20) against RSV, thus resulting comparable to or more potent than the respective reference drugs (NM108 and ribavirin). Most of these compounds derive from 2-benzylbenzimidazole, but also other molecular scaffolds [as 1-phenylbenzimidazole (2), 2-trifluoromethylbenzimidazole (69), dihydropyrido[3′,2′:4,5]imidazo[1,2-a][1,4]benzodiazepin-5-one (3), dibenzo[c,e]benzimidazo[1,2-a]azepine (22), and 2-(tetrahydropyran-2-yl)benzimidazole (81, 82 and 86)] are related to interesting levels of activity against these or other viruses (BVDV, Sb-1). Thus, these scaffolds (some of which, so far unexplored), represent valid starting points to develop more efficient agents against pathologies caused by CVB-5, RSV, BVDV and Sb-1 viruses. © 2014 Elsevier Ltd. All rights reserved.
|Titolo:||Antiviral activity of benzimidazole derivatives. III. Novel anti-CVB-5, anti-RSV and anti-Sb-1 agents|
|Parole Chiave:||Anti-CVB-5; anti-RSV, anti-Sb-1 activity; Benzimidazole derivatives; RNA and DNA viruses|
|Settore Scientifico Disciplinare:||Settore CHIM/08 - Chimica Farmaceutica|
Settore BIO/19 - Microbiologia Generale
|Data di pubblicazione:||2014|
|Digital Object Identifier (DOI):||10.1016/j.bmc.2014.06.043|
|Appare nelle tipologie:||01 - Articolo su periodico|