Targeting SARS-CoV-2 Polymerase with New Nucleoside Analogues

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 polyme...

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Bibliographic Details
Published inMolecules Vol. 26; no. 11; p. 3461
Main Authors Daikopoulou, Vasiliki, Apostolou, Panagiotis, Mourati, Sofia, Vlachou, Ioanna, Gougousi, Maria, Papasotiriou, Ioannis
Format Journal Article
LanguageEnglish
Published Basel MDPI AG 07.06.2021
MDPI
Subjects
Cancer
Coronaviruses
COVID-19
Enzymes
Fluorine
Hepatitis
nucleoside derivatives
Phosphorylation
Polymerization
quinazoline moiety
RNA polymerase
Severe acute respiratory syndrome coronavirus 2
Viruses
Online AccessGet full text
ISSN1420-3049
1433-1373
1420-3049
1433-1373
DOI10.3390/molecules26113461

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Summary: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.
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ISSN:1420-3049
1433-1373
1420-3049
1433-1373
DOI:10.3390/molecules26113461