Discovery of 4-(dimethylamino)quinazolines as potent and selective antagonists for the melanin-concentrating hormone receptor 1 |
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| Authors: | Kanuma Kosuke Omodera Katsunori Nishiguchi Mariko Funakoshi Takeo Chaki Shigeyuki Semple Graeme Tran Thuy-Anh Kramer Bryan Hsu Debbie Casper Martin Thomsen Bill Beeley Nigel Sekiguchi Yoshinori |
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| Affiliation: | Medicinal Research Laboratories, Taisho Pharmaceutical Co. Ltd, 1-403 Yoshino-cho, Kita-ku, Saitama, Saitama 331-9530, Japan. |
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| 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. |
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