Friday, October 14, 2022

Recent advances in the development of covalent inhibitors

Hyunsoo Kim,   Yoon Soo Hwang,   Mingi Kima  and  Seung Bum Park

RSC Med. Chem., 2021, 12, 1037-1045

https://doi.org/10.1039/D1MD00068C

The use of covalent inhibitors in the field of drug discovery has attracted considerable attention in the 2000s. As a result, more than 50 covalent drugs are currently on the market, and numerous covalent drug candidates are now under development. Therefore, interest in covalent drugs is expected to continue in the future. The purpose of this focused review is to provide an understanding of the development of covalent inhibitors by describing their inherent characteristics, possibilities, and limitations based on their mechanistic differences from noncovalent inhibitors. We also introduce the latest covalent warheads that can be applied to the development of potential covalent inhibitors.

Synthesis and functionalization of vinyl sulfonimidamides and their potential as electrophilic warheads

Yu Tung Wong,  Charles Bell, and  Michael C. Willis Chem. Sci., 2025 DOI https://doi.org/10.1039/D5SC02420J Covalent inhibitor design is dom...