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 , , Nigel Beeley، نويسنده , , Yoshinori Sekiguchi، نويسنده ,
Abstract :
A series of 4-(dimethylamino)quinazoline based antagonists of the melanin-concentrating hormone receptor 1 (MCH-R1) is described. This series was derived from a lead compound, AR129330, identified by HTS of a GPCR-directed library using a functional assay with a constitutively activated (CART) form of the receptor. The preliminary optimization resulted in the identification of compounds 20, 21, and 23.
