Antiviral activity of benzotriazole derivatives. 5-[4-(Benzotriazol-2-yl)phenoxy]-2,2-dimethylpentanoic acids potently and selectively inhibit Coxsackie Virus B5

作者：Loddo Roberta^*; Novelli Federica; Sparatore Anna; Tasso Bruno; Tonelli Michele; Boido Vito; Sparatore Fabio; Collu Gabriella; Delogu Ilenia; Giliberti Gabriele; La Colla Paolo

来源：Bioorganic & Medicinal Chemistry, 2015, 23(21): 7024-7034.

DOI：10.1016/j.bmc.2015.09.035

• Antiviral agents
• N-Substituted benzotriazoles
• Coxsackie Virus B5 inhibitors
• RSV inhibitors
• Anti-Flaviviridae agents

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 mu M) and the latter for the large spectrum of activity including six viruses with a mean EC50= 12 mu M. 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 mu M 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.

• 出版日期2015-11-1