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

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.
Kosuke Kanuma 1,  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
Affiliations

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.

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