Alkyne Derivatives of SARS-CoV-2 Main Protease Inhibitors Including Nirmatrelvir Inhibit by Reacting Covalently with the Nucleophilic Cysteine

著者: Lennart Brewitz, Leo Dumjahn, Yilin Zhao, David Owen, Stephen M. Laidlaw, Tika R. Malla, Dung Nguyen, Petra Lukacik, E. Salah, Adam Crawshaw, Anna J. Warren, José Trincão, Claire Strain‐Damerell, Miles W. Carroll, Martin Walsh, Christopher J. Schofield - Journal of Medicinal Chemistry 2023 被引用: 67

and other nucleophilic cysteine proteases by alkynes, which, in contrast to nitriles, can be functionalized at their terminal position to optimize inhibition and selectivity, as well as pharmacodynamic and pharmacokinetic properties.