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Targeting SARS-CoV-2 Polymerase with New Nucleoside Analogues
Authors:Vasiliki Daikopoulou  Panagiotis Apostolou  Sofia Mourati  Ioanna Vlachou  Maria Gougousi  Ioannis Papasotiriou
Institution:1.Research Genetic Cancer Centre S.A. Industrial Area of Florina, GR53100 Florina, Greece; (V.D.); (P.A.); (S.M.); (I.V.); (M.G.);2.Research Genetic Cancer Centre International GmbH, Baarerstrasse, 95, 6301 Zug, Switzerland
Abstract:Despite the fact that COVID-19 vaccines are already available on the market, there have not been any effective FDA-approved drugs to treat this disease. There are several already known drugs that through drug repositioning have shown an inhibitory activity against SARS-CoV-2 RNA-dependent RNA polymerase. These drugs are included in the family of nucleoside analogues. In our efforts, we synthesized a group of new nucleoside analogues, which are modified at the sugar moiety that is replaced by a quinazoline entity. Different nucleobase derivatives are used in order to increase the inhibition. Five new nucleoside analogues were evaluated with in vitro assays for targeting polymerase of SARS-CoV-2.
Keywords:nucleoside derivatives  COVID-19  quinazoline moiety
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