DERIVATIVES OF 4-AMINO-PYRIDINE AS SELECTIVE THROMBIN INHIBITORS

Bioorganic & Medicinal Chemistry Letters
1997.0

Abstract

During screening for novel thrombin inhibitorsit was discovered that the 4-aminopyridine derivative 1 inhibits human ct-thrombin competitively and selectively. The 4-aminopyridine moiety itself is most likely the major determinant of the selectivity due to the increased hydrophobicityof the SI pocket in thrombin compared to trypsin and plasmin. Optimization led to the selective thrombin inhibitor 14 with an inhibition constant, Ki of 70 nM.

Knowledge Graph

Similar Paper