Naphthoquinones as Covalent Reversible Inhibitors of Cysteine Proteases—Studies on Inhibition Mechanism and Kinetics

Naphthoquinones as Covalent Reversible Inhibitors of Cysteine Proteases—Studies on Inhibition Mechanism and Kinetics

The facile synthesis and detailed investigation of a class of highly potent protease inhibitors based on 1,4-naphthoquinones with a dipeptidic recognition motif (HN-l-Phe-l-Leu-OR) in the 2-position and an electron-withdrawing group (EWG) in the 3-position is presented. One of the compound represent...

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Bibliographic Details
Main Authors: Philipp Klein, Fabian Barthels, Patrick Johe, Annika Wagner, Stefan Tenzer, Ute Distler, Thien Anh Le, Paul Schmid, Volker Engel, Bernd Engels, Ute A. Hellmich, Till Opatz, Tanja Schirmeister
Format: Article
Language:English
Published: MDPI AG 2020-04-01
Series:Molecules
Subjects:
protease
rhodesain
covalent reversible inhibition
1,4-naphthoquinone
nucleophilic addition
prodrug
Online Access:https://www.mdpi.com/1420-3049/25/9/2064

Internet

https://www.mdpi.com/1420-3049/25/9/2064

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