设计、合成及二硫代氨基甲酸盐衍生物作为 SARS-CoV-2 M 抑制剂的生物评估。
Design, synthesis, and biological evaluation of dithiocarbamate derivatives as SARS-CoV-2 M inhibitors.
机构信息
School of Chemical Engineering and Pharmacy, Hubei Key Laboratory of Novel Reactor and Green Chemical Technology, Key Laboratory for Green Chemical Process of Ministry of Education, Wuhan Institute of Technology, Wuhan 430205, China.
School of Chemical Engineering and Pharmacy, Hubei Key Laboratory of Novel Reactor and Green Chemical Technology, Key Laboratory for Green Chemical Process of Ministry of Education, Wuhan Institute of Technology, Wuhan 430205, China.
出版信息
Bioorg Med Chem Lett. 2024 Dec 1;114:130011. doi: 10.1016/j.bmcl.2024.130011. Epub 2024 Oct 30.
SARS-CoV-2 continues to mutate, spread, and impact public health and daily life. The main protease (M) 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 inhibitors. Notably, compound L2 exhibited an IC value of 9.1 ± 2.0 nM against SARS-CoV-2 M, underscoring its potential as a promising candidate for anti-coronaviral therapy and justifying further research and development.
SARS-CoV-2 持续发生突变、传播，并影响公共卫生和日常生活。主蛋白酶（M）对于 SARS-CoV-2 的复制和成熟至关重要，由于其高度保守性和人体内缺乏同源蛋白酶，使其成为抗冠状病毒药物发现和开发的理想靶点。在此，我们设计并合成了一系列二硫代氨基甲酸盐衍生物，作为有效的 SARS-CoV-2 M 抑制剂。值得注意的是，化合物 L2 对 SARS-CoV-2 M 的 IC 值为 9.1±2.0 nM，突出了其作为一种有前途的抗冠状病毒治疗候选药物的潜力，值得进一步研究和开发。
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