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发现4-（二甲基氨基）喹唑啉类化合物作为黑色素浓缩激素受体1的强效和选择性拮抗剂。

Discovery of 4-(dimethylamino)quinazolines as potent and selective antagonists for the melanin-concentrating hormone receptor 1.

作者信息

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

机构信息

Medicinal Research Laboratories, Taisho Pharmaceutical Co. Ltd, 1-403 Yoshino-cho, Kita-ku, Saitama, Saitama 331-9530, Japan.

出版信息

Bioorg Med Chem Lett. 2005 May 16;15(10):2565-9. doi: 10.1016/j.bmcl.2005.03.052.

DOI:10.1016/j.bmcl.2005.03.052
PMID:15863317
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.

摘要

描述了一系列基于4-(二甲基氨基)喹唑啉的黑色素浓缩激素受体1（MCH-R1）拮抗剂。该系列源自一种先导化合物AR129330，它是通过使用具有组成型激活（CART）形式受体的功能测定法对GPCR导向文库进行高通量筛选（HTS）鉴定出来的。初步优化导致鉴定出化合物20、21和23。

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