A library of 64 benzotriazole derivatives (17 of which were [4-(benzotriazol-2-yl)phenoxy]alkanoic acids) were screened for antiviral activity against a panel of twelve DNA and RNA viruses. Twenty-six compounds (12 of which were [4-(benzotriazol-2-yl)phenoxy]alkanoic acids) displayed activity against one or more viruses. CVB-5, RSV, BVDV, Sb-1 and YFV were, in decreasing order, the more frequently and effectively affected viruses; DENV-2, WNV, HIV-1 and Reo-1 were only occasionally and modestly affected, while the remaining viruses were not affected by any of the tested compounds. Worth of note were compounds 33 and 35; the former for the activity against Sb-1 (EC50 = 7 μM) and the latter for the large spectrum of activity including six viruses with a mean EC50 = 12 μM. Even more interesting were the alkanoic acids 45-48 and 50-57 for their activity against RSV and/or CVB-5. In particular, compound 56 displayed a potent and selective activity against CVB-5 with EC50 = 0.15 μM and SI = 100, thus representing a valuable hit compound for the development of antiviral agents for the treatment of human pathologies related to this virus.
Antiviral activity of benzotriazole derivatives : 5-[4-(Benzotriazol-2-yl)phenoxy]-2,2-dimethylpentanoic acids potently and selectively inhibit Coxsackie Virus B5 / R. Loddo, F. Novelli, A. Sparatore, B. Tasso, M. Tonelli, V. Boido, F. Sparatore, G. Collu, I. Delogu, G. Giliberti, P. La Colla. - In: BIOORGANIC & MEDICINAL CHEMISTRY. - ISSN 0968-0896. - 23:21(2015 Nov 01), pp. 7024-7034.
|Titolo:||Antiviral activity of benzotriazole derivatives : 5-[4-(Benzotriazol-2-yl)phenoxy]-2,2-dimethylpentanoic acids potently and selectively inhibit Coxsackie Virus B5|
|Parole Chiave:||Anti-Flaviviridae agents; Antiviral agents; Coxsackie Virus B5 inhibitors; N-Substituted benzotriazoles; RSV inhibitors; Biochemistry; Clinical Biochemistry; Molecular Biology; Molecular Medicine; Organic Chemistry; Drug Discovery3003 Pharmaceutical Science; 3003|
|Settore Scientifico Disciplinare:||Settore CHIM/08 - Chimica Farmaceutica|
|Data di pubblicazione:||1-nov-2015|
|Data ahead of print / Data di stampa:||25-set-2015|
|Digital Object Identifier (DOI):||http://dx.doi.org/10.1016/j.bmc.2015.09.035|
|Appare nelle tipologie:||01 - Articolo su periodico|