Lead optimization of 4-(dimethylamino)quinazolines, potent and selective antagonists for the melanin-concentrating hormone receptor 1

The synthesis and SAR of 4-(dimethylamino)quinazolines as melanin-concentrating hormone receptor 1 (MCH-R1) antagonists are reported, leading to the discovery of ATC0175. The optimization of a series of 4-(dimethylamino)quinazoline antagonists of the melanin-concentrating hormone receptor 1 (MCH-R1)...

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Bibliographic Details
Published in:	Bioorganic & medicinal chemistry letters Vol. 15; no. 17; pp. 3853 - 3856
Main Authors:	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
Format:	Journal Article
Language:	English
Published:	Oxford Elsevier Ltd 01-09-2005 Elsevier
Subjects:	ATC0175 Biological and medical sciences Hormones. Endocrine system Humans Inhibitory Concentration 50 MCH-R1 antagonists Medical sciences Melanin-concentrating hormone receptor 1 antagonists Pharmacology. Drug treatments Quinazolines - chemical synthesis Quinazolines - chemistry Quinazolines - pharmacology Radioligand Assay Receptors, Somatostatin - antagonists & inhibitors Structure-Activity Relationship Substrate Specificity Melanin-concentrating hormone receptor 1 antagonists MCH-R1 antagonists ATC0175 Cyclohexane derivatives Spacer arm Quinazoline derivatives Selectivity Optimization Structure activity relation Hydrochlorides Organic fluorine compounds Melanin concentrating hormone Benzamide derivatives Carboxamide Antagonist Chemical synthesis Biological receptor Hormonal receptor
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