Synthesis of novel substituted pyridines as inhibitors of endothelin converting enzyme-1 (ECE-1).
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.
Massa
M A
MA
Medicinal Chemistry Department, Parke-Davis Pharmaceutical Research Division, Warner-Lambert Company, Ann Arbor, MI 48105, USA.
Patt
W C
WC
Ahn
K
K
Sisneros
A M
AM
Herman
S B
SB
Doherty
A
A
D000818:Animals; D016282:Aspartic Acid Endopeptidases / Q000037:antagonists & inhibitors*; D016466:CHO Cells; D006224:Cricetinae; D000072396:Endothelin-Converting Enzymes; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D007202:Indicators and Reagents; D007700:Kinetics; D008666:Metalloendopeptidases / Q000037:antagonists & inhibitors; D010165:Palladium; D011480:Protease Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011725:Pyridines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011994:Recombinant Proteins / Q000037:antagonists & inhibitors; D013329:Structure-Activity Relationship; D014162:Transfection
D004791:Enzyme Inhibitors; D007202:Indicators and Reagents; D011480:Protease Inhibitors; D011725:Pyridines; D011994:Recombinant Proteins; D010165:Palladium; D016282:Aspartic Acid Endopeptidases; D008666:Metalloendopeptidases; C000606923:ECE1 protein, human; D000072396:Endothelin-Converting Enzymes