Design, synthesis, and biological evaluation of dithiocarbamate derivatives as SARS-CoV-2 M pro inhibitors

被引：0
|
作者：
Peng, Jin-Qi [1 ]
Xiao, Ya-Qi [1 ]
Long, Jiao [1 ]
Zhang, Shuang-Shuang [1 ]
Zhu, Yuan-Yuan [2 ]
Gu, Shuang-Xi [1 ]
机构：
[1] Wuhan Inst Technol, Sch Chem Engn & Pharm, Hubei Key Lab Novel Reactor & Green Chem Technol, Wuhan 430205, Peoples R China
[2] Wuhan Inst Technol, Sch Chem & Environm Engn, Wuhan 430205, Peoples R China
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2024年 / 114卷
关键词：
SARS-CoV-2; Main protease; Dithiocarbamates derivatives; Drug design;
D O I：
10.1016/j.bmcl.2024.130011
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
SARS-CoV-2 continues to mutate, spread, and impact public health and daily life. The main protease (Mpro) is essential for the replication and maturation of SARS-CoV-2, making it an ideal target for anti-coronaviral drug discovery and development due to its high conservation and lack of homologous proteases in humans. Herein, we designed and synthesized a series of dithiocarbamate derivatives as potent SARS-CoV-2 M pro inhibitors. Notably, compound L2 exhibited an IC50 value of 9.1 +/- 2.0 nM against SARS-CoV-2 M pro , underscoring its potential as a promising candidate for anti-coronaviral therapy and justifying further research and development.
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页数：5
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