Synthesis of novel substituted pyridines as inhibitors of endothelin converting enzyme-1 (ECE-1)

Bioorg Med Chem Lett. 1998 Aug 18;8(16):2117-22. doi: 10.1016/s0960-894x(98)00375-8.

Abstract

A series of bi-aryl pyridine carboxylic acids has been prepared and evaluated as inhibitors of ECE-1. The analogs were prepared by Pd catalyzed cross couplings of halogenated pyridines with heteroaryl organo-boranes, -tinate or -zincate derivatives.

MeSH terms

  • Animals
  • Aspartic Acid Endopeptidases / antagonists & inhibitors*
  • CHO Cells
  • Cricetinae
  • Endothelin-Converting Enzymes
  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology
  • Humans
  • Indicators and Reagents
  • Kinetics
  • Metalloendopeptidases / antagonists & inhibitors
  • Palladium
  • Protease Inhibitors / chemical synthesis*
  • Protease Inhibitors / chemistry
  • Protease Inhibitors / pharmacology
  • Pyridines / chemical synthesis*
  • Pyridines / chemistry
  • Pyridines / pharmacology
  • Recombinant Proteins / antagonists & inhibitors
  • Structure-Activity Relationship
  • Transfection

Substances

  • Enzyme Inhibitors
  • Indicators and Reagents
  • Protease Inhibitors
  • Pyridines
  • Recombinant Proteins
  • Palladium
  • Aspartic Acid Endopeptidases
  • Metalloendopeptidases
  • ECE1 protein, human
  • Endothelin-Converting Enzymes