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.

引用

页数：5

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