Abstract
Many inhibitors of enzymes have been designed by replacing the scissile amide bond in a substrate with a hydrolytically stable functionality, such as hydroxyethylene [1]. The hydroxyethylene (HET) dipeptide isostere serves as a “transition state” inhibitor and mimics the tetrahedral intermediate formed during hydrolysis (Figure 1) [2].KeywordsTransition StateCarbonyl OxygenHydroxy AcidMechanistic InsightNucleophilic AdditionThese keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.
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