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

ID: ALA1132080

Journal: Bioorg Med Chem Lett

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

Authors: Reiner JE, Lim-Wilby MS, Brunck TK, Ha-Uong T, Goldman EA, Abelman MA, Nutt RF, Semple JE, Tamura SY.

Abstract: 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.

CiteXplore: 10206557

DOI: 10.1016/s0960-894x(99)00102-x

Patent ID: ┄