Efficient diastereoselective synthesis of a hydroxyethylene dipeptide isostere

摘要

Many inhibitors of enzymes have been designed by replacing the scissile amide bond in a substrate with a hydrolytically stable functionality,such as hydroxyethylene.The hydroxyethylene (HET) dipeptide isostere serves as a "transition state" inhibitor and mimics the tetrahedral intermediate formed during hydrolysis (Figure 1).