Investigation of the S-3 site of thrombin: Design, synthesis and biological activity of 4-substituted 3-amino-2-pyridones incorporating P-1-argininals

A novel scaffold for P-4-P-2 dipeptide mimics containing a rigid pyridone s pacer was designed based on a virtual library strategy. Several selected no npeptidic 4-aralkyl or 4-alkylpyridones incorporating a P-1- argininal sequ ence were prepared. The modeling studies, synthesis and biological activiti es of these unique pyridone derivatives are reported herein. (C) 1999 Elsev ier Science Ltd. All rights reserved.