| Literature DB >> 29859999 |
Gleb V Proskurin1, Alexey A Orlov2, Vladimir A Brylev1, Liubov I Kozlovskaya3, Alexey A Chistov4, Galina G Karganova5, Vladimir A Palyulin6, Dmitry I Osolodkin7, Vladimir A Korshun8, Andrey V Aralov1.
Abstract
A series of analogues of potent antiviral perylene nucleoside dUY11 with methylthiomethyl (MTM), azidomethyl (AZM) and HO-C1-4-alkyl-1,2,3-triazol-1,4-diyl groups at 3'-O-position as well as the two products of copper-free alkyne-azide cycloaddition of the AZM derivative were prepared and evaluated against tick-borne encephalitis virus (TBEV). Four compounds (4, 6, 8a, 8b) showed EC50 ≤ 10 nM, thus appearing the most potent TBEV inhibitors to date. Moreover, these nucleosides have higher lipophilicity (clogP) and increased solubility in aq. DMSO vs. parent compound dUY11.Entities:
Keywords: Antiviral activity; Cycloaddition; Lipophilicity; Nucleoside; Tick-borne encephalitis virus
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Year: 2018 PMID： 29859999 DOI： 10.1016/j.ejmech.2018.05.040
Source DB: PubMed Journal: Eur J Med Chem ISSN： 0223-5234 Impact factor: 6.514