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

Author:

Stalinskaya Alena L.ORCID,Martynenko Nadezhda V.,Shulgau Zarina T.ORCID,Shustov Alexandr V.ORCID,Keyer Viktoriya V.,Kulakov Ivan V.ORCID

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.

Funder

Ministry of Education and Science of the Republic of Kazakhstan

Publisher

MDPI AG

Subject

Chemistry (miscellaneous),Analytical Chemistry,Organic Chemistry,Physical and Theoretical Chemistry,Molecular Medicine,Drug Discovery,Pharmaceutical Science

Reference48 articles.

1. The emergence, genomic diversity and global spread of SARS-CoV-2

2. The Emergency Use Authorization of Pharmaceuticals: History and Utility During the COVID-19 Pandemic

3. COVID-19 updates: Remdesivir (Veklury) in high-risk outpatients with COVID-19;Med. Lett. Drugs Ther.,2022

4. COVID-19 updates: NIH outpatient treatment guidelines;Med. Lett. Drugs Ther.,2022

5. US201 Study: A Phase 2, Randomized Proof-of-Concept Trial of Favipiravir for the Treatment of COVID-19

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