中文版 | English
Title

Synthesis of deuterated S-217622 (Ensitrelvir) with antiviral activity against coronaviruses including SARS-CoV-2

Author
Corresponding AuthorZhang,Hongmin; Guo,Deyin; Li,Yingjun; Zhang,Xumu
Joint first authorYang,Yujian; Cao,Liu; Yan,Ming
Publication Years
2023-05-01
DOI
Source Title
ISSN
0166-3542
EISSN
1872-9096
Volume213
Abstract

S-217622 (Ensitrelvir) is a reversible severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) 3-chymotrypsin-like protease (3CL) inhibitor which obtained emergency regulatory approval in Japan for the treatment of SARS-CoV-2 infection on Nov 22, 2022. Herein, analogs of S-271622 with deuterium-for-hydrogen replacement were synthesized for comparison of the antiviral activities and pharmacokinetic (PK) profiles. Compared to the parent compound, C11-d2-S-217622 compound YY-278 retained in vitro activity against 3CL and SARS-CoV-2. X-ray crystal structural studies showed similar interactions of SARS-CoV-2 3CL with YY-278 and S-271622. The PK profiling revealed the relatively favorable bioavailability and plasma exposure of YY-278. In addition, YY-278, as well as S-217622, displayed broadly anti-coronaviral activities against 6 other coronaviruses that infect humans and animals. These results laid the foundation for further research on the therapeutic potential of YY-278 against COVID-19 and other coronaviral diseases.

Keywords
URL[Source Record]
Indexed By
Language
English
SUSTech Authorship
First ; 共同第一 ; Corresponding
Funding Project
Basic and Applied Basic Research Foundation of Guangdong Province[2020A1515110361] ; Department of Education of Guangdong Province[2022KTSCX107] ; National Natural Science Foundation of China[82150206] ; National Natural Science Foundation of China[82204194] ; National Natural Science Foundation of China[82230075] ; Shenzhen Graduate School, Peking University[JCYJ20220530113609021] ; Shenzhen Graduate School, Peking University[JSGG20210901145403012] ; Shenzhen Graduate School, Peking University[KQTD20180411143323605]
ESI Research Field
PHARMACOLOGY & TOXICOLOGY
Scopus EID
2-s2.0-85151519226
Data Source
Scopus
Citation statistics
Cited Times [WOS]:0
Document TypeJournal Article
Identifierhttp://kc.sustech.edu.cn/handle/2SGJ60CL/524145
DepartmentDepartment of Chemistry
生命科学学院
理学院
前沿与交叉科学研究院
生命科学学院_生物系
Affiliation
1.Department of Chemistry,College of Science,Academy for Advanced Interdisciplinary Studies,and Medi-X Pingshan,Southern University of Science and Technology,Shenzhen,Guangdong,518000,China
2.Centre for Infection and Immunity Studies (CIIS),School of Medicine,Sun Yat-sen University,Shenzhen,Guangdong,518107,China
3.Department of Biology,School of Life Sciences,Southern University of Science and Technology,Shenzhen,Guangdong,518000,China
4.Guangzhou Laboratory,Bio-island,Guangzhou,Guangdong,510320,China
5.Guangdong Province Key Laboratory of Laboratory Animals,Guangdong Laboratory Animals Monitoring Institute,Guangzhou,Guangdong,510663,China
First Author AffilicationDepartment of Chemistry;  Academy for Advanced Interdisciplinary Studies;  College of Science
Corresponding Author AffilicationDepartment of Biology;  School of Life Sciences;  Department of Chemistry;  Academy for Advanced Interdisciplinary Studies;  College of Science
First Author's First AffilicationDepartment of Chemistry;  Academy for Advanced Interdisciplinary Studies;  College of Science
Recommended Citation
GB/T 7714
Yang,Yujian,Cao,Liu,Yan,Ming,et al. Synthesis of deuterated S-217622 (Ensitrelvir) with antiviral activity against coronaviruses including SARS-CoV-2[J]. Antiviral Research,2023,213.
APA
Yang,Yujian.,Cao,Liu.,Yan,Ming.,Zhou,Jun.,Yang,Sidi.,...&Zhang,Xumu.(2023).Synthesis of deuterated S-217622 (Ensitrelvir) with antiviral activity against coronaviruses including SARS-CoV-2.Antiviral Research,213.
MLA
Yang,Yujian,et al."Synthesis of deuterated S-217622 (Ensitrelvir) with antiviral activity against coronaviruses including SARS-CoV-2".Antiviral Research 213(2023).
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