共价键
酶
化学
蛋白酶
病毒学
病毒复制
严重急性呼吸综合征冠状病毒2型(SARS-CoV-2)
半胱氨酸蛋白酶
抗病毒药物
冠状病毒
生物化学
病毒
2019年冠状病毒病(COVID-19)
药理学
体外
生物
医学
传染病(医学专业)
有机化学
病理
疾病
作者
Julia Stille,Jevgenijs Tjutrins,Guanyu Wang,Felipe A. Venegas,Christopher Hennecker,Andres Mauricio Rueda,Itai Sharon,Nicole Blaine,Caitlin E. Miron,Sharon Pinus,Anne Labarre,Jessica Plescia,Mihai Burai Patrascu,Xiaocong Zhang,Alexander S. Wahba,Danielle Vlaho,Mitchell Huot,T.M. Schmeing,Anthony Mittermaier,Nicolas Moitessier
标识
DOI:10.1016/j.ejmech.2021.114046
摘要
Severe diseases such as the ongoing COVID-19 pandemic, as well as the previous SARS and MERS outbreaks, are the result of coronavirus infections and have demonstrated the urgent need for antiviral drugs to combat these deadly viruses. Due to its essential role in viral replication and function, 3CLpro (main coronaviruses cysteine-protease) has been identified as a promising target for the development of antiviral drugs. Previously reported SARS-CoV 3CLpro non-covalent inhibitors were used as a starting point for the development of covalent inhibitors of SARS-CoV-2 3CLpro. We report herein our efforts in the design and synthesis of submicromolar covalent inhibitors when the enzymatic activity of the viral protease was used as a screening platform.
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