Bioorganic and Medicinal Chemistry Letters p. 3853 - 3856 (2005)
Update date:2022-08-05
Topics:
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
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.
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