期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 15, 期 17, 页码 3853-3856出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2005.05.121
关键词
melanin-concentrating hormone receptor 1 antagonists; MCH-R1 antagonists; ATC0175
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 alpha(2A) receptors. (c) 2005 Elsevier Ltd. All rights reserved.
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