Academic Journal
Antiviral activity of benzotriazole derivatives : 5-[4-(Benzotriazol-2-yl)phenoxy]-2,2-dimethylpentanoic acids potently and selectively inhibit Coxsackie Virus B5
| العنوان: | Antiviral activity of benzotriazole derivatives : 5-[4-(Benzotriazol-2-yl)phenoxy]-2,2-dimethylpentanoic acids potently and selectively inhibit Coxsackie Virus B5 |
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| المؤلفون: | R. Loddo, F. Novelli, B. Tasso, M. Tonelli, V. Boido, F. Sparatore, G. Collu, I. Delogu, G. Giliberti, P. La Colla, A. Sparatore |
| المساهمون: | R. Loddo, F. Novelli, A. Sparatore, B. Tasso, M. Tonelli, V. Boido, F. Sparatore, G. Collu, I. Delogu, G. Giliberti, P. La Colla |
| بيانات النشر: | Elsevier |
| سنة النشر: | 2015 |
| المجموعة: | The University of Milan: Archivio Istituzionale della Ricerca (AIR) |
| مصطلحات موضوعية: | Anti-Flaviviridae agent, Antiviral agent, Coxsackie Virus B5 inhibitor, N-Substituted benzotriazole, RSV inhibitor, Biochemistry, Clinical Biochemistry, Molecular Biology, Molecular Medicine, Organic Chemistry, Drug Discovery3003 Pharmaceutical Science, Settore CHIM/08 - Chimica Farmaceutica |
| Time: | 3003 |
| الوصف: | 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. |
| نوع الوثيقة: | article in journal/newspaper |
| اللغة: | English |
| Relation: | info:eu-repo/semantics/altIdentifier/pmid/26443549; info:eu-repo/semantics/altIdentifier/wos/WOS:000364437400025; volume:23; issue:21; firstpage:7024; lastpage:7034; numberofpages:11; journal:BIOORGANIC & MEDICINAL CHEMISTRY; http://hdl.handle.net/2434/337178; info:eu-repo/semantics/altIdentifier/scopus/2-s2.0-84946115033 |
| DOI: | 10.1016/j.bmc.2015.09.035 |
| الاتاحة: | http://hdl.handle.net/2434/337178 https://doi.org/10.1016/j.bmc.2015.09.035 |
| رقم الانضمام: | edsbas.909E179 |
| قاعدة البيانات: | BASE |
| DOI: | 10.1016/j.bmc.2015.09.035 |
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