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

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

  • Bioorg Med Chem. 2015 Nov 1;23(21):7024-34. doi: 10.1016/j.bmc.2015.09.035.
Roberta Loddo 1,  Federica Novelli 2,  Anna Sparatore 3,  Bruno Tasso 2,  Michele Tonelli 4,  Vito Boido 2,  Fabio Sparatore 2,  Gabriella Collu 5,  Ilenia Delogu 5,  Gabriele Giliberti 5,  Paolo La Colla 5
Affiliations

Affiliations

  • 1 Dipartimento di Scienze Biomediche, Università degli Studi di Cagliari, Cittadella Universitaria, 09042 Monserrato (CA), Italy. Electronic address: rloddo@unica.it.
  • 2 Dipartimento di Farmacia, Università degli Studi di Genova, Viale Benedetto XV, 3, 16132 Genova, Italy.
  • 3 Dipartimento di Scienze Farmaceutiche, Università degli Studi di Milano, Via Mangiagalli 25, 20133 Milano, Italy.
  • 4 Dipartimento di Farmacia, Università degli Studi di Genova, Viale Benedetto XV, 3, 16132 Genova, Italy. Electronic address: michele.tonelli@unige.it.
  • 5 Dipartimento di Scienze Biomediche, Università degli Studi di Cagliari, Cittadella Universitaria, 09042 Monserrato (CA), Italy.
PMID: 26443549 DOI: 10.1016/j.bmc.2015.09.035
Abstract

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.

Keywords

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

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