Discovery of tetralin ureas as potent melanin concentrating hormone 1 receptor antagonists.
Melanin concentrating hormone (MCH) plays an important role in the regulation of food intake and energy balance in mammals. MCH-1 receptor (MCH1R) deficient mice are lean and resistant to diet-induced obesity. As such, MCH1R antagonists are believed to have potential as possible treatments for obesity. The discovery of a novel class of tetralin ureas as potent MCH1R antagonists is described herein.
Guo
Tao
T
Pharmacopeia Drug Discovery Inc., PO Box 5350, Princeton, NJ 08543-5350, USA. tguo@pcop.com
Gu
Huizhong
H
Hobbs
Doug W
DW
Busler
Dennis E
DE
Rokosz
Laura L
LL
D000818:Animals; D001667:Binding, Competitive / Q000187:drug effects; D016466:CHO Cells; D006224:Cricetinae; D003412:Cricetulus; D015195:Drug Design; D006801:Humans; D051379:Mice; D018345:Mice, Knockout; D051381:Rats; D017481:Receptors, Somatostatin / Q000037:antagonists & inhibitors* / Q000235:genetics; D013329:Structure-Activity Relationship; D013764:Tetrahydronaphthalenes / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology*; D014018:Tissue Distribution; D014508:Urea / Q000031:analogs & derivatives* / Q000493:pharmacokinetics / Q000494:pharmacology*
C491209:Mchr1 protein, mouse; D017481:Receptors, Somatostatin; D013764:Tetrahydronaphthalenes; D014508:Urea