title: Discovery of 4-(dimethylamino)quinazolines as potent and selective antagonists for the melanin-concentrating hormone receptor 1.
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.
authors.affiliation: Medicinal Research Laboratories, Taisho Pharmaceutical Co. Ltd, 1-403 Yoshino-cho, Kita-ku, Saitama, Saitama 331-9530, Japan.
authors.forename: Kosuke
authors.initials: K
authors.lastname: Kanuma
authors.forename: Katsunori
authors.initials: K
authors.lastname: Omodera
authors.forename: Mariko
authors.initials: M
authors.lastname: Nishiguchi
authors.forename: Takeo
authors.initials: T
authors.lastname: Funakoshi
authors.forename: Shigeyuki
authors.initials: S
authors.lastname: Chaki
authors.forename: Graeme
authors.initials: G
authors.lastname: Semple
authors.forename: Thuy-Anh
authors.initials: TA
authors.lastname: Tran
authors.forename: Bryan
authors.initials: B
authors.lastname: Kramer
authors.forename: Debbie
authors.initials: D
authors.lastname: Hsu
authors.forename: Martin
authors.initials: M
authors.lastname: Casper
authors.forename: Bill
authors.initials: B
authors.lastname: Thomsen
authors.forename: Nigel
authors.initials: N
authors.lastname: Beeley
authors.forename: Yoshinori
authors.initials: Y
authors.lastname: Sekiguchi
mesh_terms: D002460:Cell Line; D006801:Humans; D011799:Quinazolines / Q000737:chemistry* / Q000494:pharmacology*; D011979:Receptors, Pituitary Hormone / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: D011799:Quinazolines; D011979:Receptors, Pituitary Hormone; C092274:melanin-concentrating hormone receptor