Title | Synthesis of deuterated S-217622 (Ensitrelvir) with antiviral activity against coronaviruses including SARS-CoV-2 |
Author | |
Corresponding Author | Zhang,Hongmin; Guo,Deyin; Li,Yingjun; Zhang,Xumu |
Joint first author | Yang,Yujian; Cao,Liu; Yan,Ming |
Publication Years | 2023-05-01
|
DOI | |
Source Title | |
ISSN | 0166-3542
|
EISSN | 1872-9096
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Volume | 213 |
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]
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ESI Research Field | PHARMACOLOGY & TOXICOLOGY
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Scopus EID | 2-s2.0-85151519226
|
Data Source | Scopus
|
Citation statistics |
Cited Times [WOS]:0
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Document Type | Journal Article |
Identifier | http://kc.sustech.edu.cn/handle/2SGJ60CL/524145 |
Department | Department 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 Affilication | Department of Chemistry; Academy for Advanced Interdisciplinary Studies; College of Science |
Corresponding Author Affilication | Department of Biology; School of Life Sciences; Department of Chemistry; Academy for Advanced Interdisciplinary Studies; College of Science |
First Author's First Affilication | Department 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.
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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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