195877-56-6Relevant articles and documents
Solution-phase and solid-phase synthesis of novel transition state inhibitors of coagulation enzymes incorporating a piperidinyl moiety
Adang, Anton E. P.,Peters, Co A. M.,Gerritsma, Siene,De Zwart, Edwin,Veeneman, Gerrit
, p. 1227 - 1232 (2007/10/03)
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.
