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Synthesis and Antiviral Properties against SARS-CoV-2 of Epoxybenzooxocino[4,3-b]Pyridine Derivatives

Alena L. Stalinskaya, Nadezhda V. Martynenko, Zarina Shulgau, Alexandr V. Shustov, Viktoriya Keyer, И. В. Кулаков

2022Molecules20 citationsDOIOpen Access PDF

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.

Topics & Concepts

Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2)PyridineVirologyCoronavirus disease 2019 (COVID-19)2019-20 coronavirus outbreakChemistryStereochemistryBiologyMedicineMedicinal chemistryInfectious disease (medical specialty)OutbreakDiseasePathologySynthesis and biological activitySynthesis and Biological EvaluationCancer therapeutics and mechanisms