Author/Authors :
Kosuke Kanuma، نويسنده , , Katsunori Omodera، نويسنده , , Mariko Nishiguchi، نويسنده , , Takeo Funakoshi، نويسنده , , Shigeyuki Chaki، نويسنده , , Graeme Semple، نويسنده , , Thuy-Anh Tran، نويسنده , , Bryan Kramer، نويسنده , , Debbie Hsu، نويسنده , , Martin Casper، نويسنده , , Bill Thomsen، نويسنده , , Yoshinori Sekiguchi، نويسنده ,
Abstract :
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.
