Biaryl diamides as potent melanin concentrating hormone receptor 1 antagonists.
Herein, we report the discovery of the potent and selective biaryl diamide derived MCH-R1 receptor antagonist 1, which was identified upon modification of a previously disclosed biaryl urea series. This paper describes one of the strategies incorporated to remove the highly mutagenic biarylaniline present in an otherwise promising biaryl urea series.
Palani
Anandan
A
Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. anandan.palani@spcorp.com
Shapiro
Sherry
S
McBriar
Mark D
MD
Clader
John W
JW
Greenlee
William J
WJ
O'Neill
Kim
K
Hawes
Brian
B
D000577:Amides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D017481:Receptors, Somatostatin / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D014508:Urea / Q000737:chemistry
D000577:Amides; C103263:MCHR1 protein, human; D017481:Receptors, Somatostatin; D014508:Urea