Sy. Tamura et al., DESIGN AND SYNTHESIS OF A NOVEL CLASS OF THROMBIN INHIBITORS INCORPORATING HETEROCYCLIC DIPEPTIDE SURROGATES, Bioorganic & medicinal chemistry letters, 7(12), 1997, pp. 1543-1548
Several potent and selective inhibitors of thrombin incorporating nove
l 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 s
ynthesis and biological activities of these unique aromatic heterocycl
ic derivatives are reported herein. (C) 1997 Elsevier Science Ltd.