Design and synthesis of a novel class of thrombin inhibitors incorporating heterocyclic dipeptide surrogates

Abstract

Several potent and selective inhibitors of thrombin incorporating novel heterocyclic peptide surrogates in the P 3-P 2 position of peptidyl argininals have been discovered. Illustrated in this article are three classes of heterocycles: pyridones, uracils, and pyrimidinones. The synthesis and biological activities of these unique aromatic heterocyclic derivatives are reported herein.