Investigation of the S3 site of thrombin: Design, synthesis and biological activity of 4-substituted 3-amino-2-pyridones incorporating P1- argininals

Article abstract of DOI:10.1016/S0960-894X(99)00102-X

A novel scaffold for P₄-P₂ dipeptide mimics containing a rigid pyridone spacer was designed based on a virtual library strategy. Several selected nonpeptidic 4-aralkyl or 4-alkylpyridones incorporating a P₁- argininal sequence were prepared. The modeling studies, synthesis and biological activities of these unique pyridone derivatives are reported herein.