Author/Authors :
Joseph Cacciola، نويسنده , , John M. Fevig، نويسنده , , Richard S. Alexander، نويسنده , , David R. Brittelli، نويسنده , , Charles A. Kettner، نويسنده , , Robert M. Knabb، نويسنده , , Patricia C. Weber، نويسنده ,
Abstract :
A series of boropeptide thrombin inhibitors was prepared in which the P3 residues of 2 (Ac-(D)-Phe-Pro-boroLys-OH • HCl) and 3 (3-Phenylpropionyl-Pro-boroLys-OH • HCl) were replaced by conformationally-restricted, benzoic acid-derived residues 4. The potent binding affinity of the resulting inhibitors such as 10 may be due in part to a unique mode of binding in the thrombin active site.
