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Synthesis and Antiviral Properties against SARS-CoV-2 of Epoxybenzooxocino[4,3-b]Pyridine Derivatives
Authors:Alena L. Stalinskaya  Nadezhda V. Martynenko  Zarina T. Shulgau  Alexandr V. Shustov  Viktoriya V. Keyer  Ivan V. Kulakov
Affiliation:1.Institute of Chemistry, Tyumen State University, 15a Perekopskaya St., 625003 Tyumen, Russia; (A.L.S.); (N.V.M.);2.National Center for Biotechnology, 13/5 Kurgalzhynskoe road, Nur-Sultan 010000, Kazakhstan; (Z.T.S.); (A.V.S.); (V.V.K.)
Abstract:The COVID-19 pandemic is ongoing as of mid-2022 and requires the development of new therapeutic drugs, because the existing clinically approved drugs are limited. In this work, seven derivatives of epoxybenzooxocinopyridine were synthesized and tested for the ability to inhibit the replication of the SARS-CoV-2 virus in cell cultures. Among the described compounds, six were not able to suppress the SARS-CoV-2 virus’ replication. One compound, which is a derivative of epoxybenzooxocinopyridine with an attached side group of 3,4-dihydroquinoxalin-2-one, demonstrated antiviral activity comparable to that of one pharmaceutical drug. The described compound is a prospective lead substance, because the half-maximal effective concentration is 2.23 μg/μL, which is within a pharmacologically achievable range.
Keywords:epoxybenzooxocinopyridine derivatives   antiviral activity   SARS-CoV-2
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