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

M A Massa; W C Patt; K Ahn; A M Sisneros; S B Herman; A Doherty

doi:10.1016/s0960-894x(98)00375-8

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.

Authors

M A Massa¹, W C Patt, K Ahn, A M Sisneros, S B Herman, A Doherty

Affiliation

¹ Medicinal Chemistry Department, Parke-Davis Pharmaceutical Research Division, Warner-Lambert Company, Ann Arbor, MI 48105, USA.

PMID: 9873497
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