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

Kosuke Kanuma; Katsunori Omodera; Mariko Nishiguchi; Takeo Funakoshi; Shigeyuki Chaki; Graeme Semple; Thuy-Anh Tran; Bryan Kramer; Debbie Hsu; Martin Casper; Bill Thomsen; Nigel Beeley; Yoshinori Sekiguchi

doi:10.1016/j.bmcl.2005.03.052

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

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

Authors

Kosuke Kanuma¹, Katsunori Omodera, Mariko Nishiguchi, Takeo Funakoshi, Shigeyuki Chaki, Graeme Semple, Thuy-Anh Tran, Bryan Kramer, Debbie Hsu, Martin Casper, Bill Thomsen, Nigel Beeley, Yoshinori Sekiguchi

Affiliation

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

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

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.

MeSH terms

Cell Line
Humans
Quinazolines / chemistry*
Quinazolines / pharmacology*
Receptors, Pituitary Hormone / antagonists & inhibitors*
Structure-Activity Relationship

Substances

Quinazolines
Receptors, Pituitary Hormone
melanin-concentrating hormone receptor