509142-46-5Relevant articles and documents
Lead optimization of 4-(dimethylamino)quinazolines, potent and selective antagonists for the melanin-concentrating hormone receptor 1
Kanuma, Kosuke,Omodera, Katsunori,Nishiguchi, Mariko,Funakoshi, Takeo,Chaki, Shigeyuki,Semple, Graeme,Tran, Thuy-Anh,Kramer, Bryan,Hsu, Debbie,Casper, Martin,Thomsen, Bill,Sekiguchi, Yoshinori
, p. 3853 - 3856 (2005)
The optimization of a series of 4-(dimethylamino)quinazoline antagonists of the melanin-concentrating hormone receptor 1 (MCH-R1) is described. The combination of the elaboration of both the linker portion and the terminal phenyl ring provided N-(cis-4-{[4-(dimethylamino)quinazolin-2-yl]amino} cyclohexyl)-3,4-difluorobenzamide hydrochloride 28 (ATC0175), which showed excellent antagonist activity at the MCH-R1 (IC50 = 3.4 nM) as well as good selectivity over the Y5 and the α2A receptors.