Bioorganic and Medicinal Chemistry Letters p. 1227 - 1232 (1999)
Update date:2022-08-03
Topics:
Adang, Anton E. P.
Peters, Co A. M.
Gerritsma, Siene
De Zwart, Edwin
Veeneman, Gerrit
2-Amino-3-piperidin-4-yl-propionic acid containing peptidomimetics are potent protease inhibitors when combined with an appropriate keto-thiazole or keto-carboxylic acid moiety. A novel P1 residue in factor Xa and thrombin inhibitors has been found resulting in IC50 values as low as 0.048 μM, a factor of ten more potent than Argatroban. Starting with non-chiral synthetic routes, a new stereospecific route was developed as well as a new solid- phase method.
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