| Literature DB >> 33322151 |
Gabriela Brzuska1, Gabriela Pastuch-Gawolek2,3, Monika Krawczyk2,3, Boguslaw Szewczyk1, Ewelina Krol1.
Abstract
Tick-borne encephalitis virus (TBEV) transmitted by ticks is a pathogen of great medical importance. As still no effective antiviral treatment is available, in the present study, a series of uridine glycoconjugates containing amide or/and 1,2,3-triazole moiety in the linker structure was synthesized and evaluated for the antiviral activity against two strains of TBEV: a highly virulent Hypr strain and less virulent Neudoerfl strain, using standardized previously in vitro assays. Our data have shown that four compounds from the series (18-21) possess strong activity against both TBEV strains. The half maximal inhibitory concentration (IC50) values of compounds 18-21 were between 15.1 and 3.7 μM depending on the virus strain, which along with low cytotoxicity resulted in high values of the selectivity index (SI). The obtained results suggest that these compounds may be promising candidates for further development of new therapies against flaviviruses.Entities:
Keywords: antiviral activity; flavivirus; glycosyltransferase inhibitors; tick-borne encephalitis virus; uridine glycoconjugates
Year: 2020 PMID: 33322151 PMCID: PMC7764612 DOI: 10.3390/ph13120460
Source DB: PubMed Journal: Pharmaceuticals (Basel) ISSN: 1424-8247