Literature DB >> 15863317

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

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.   

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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Year:  2005        PMID: 15863317     DOI: 10.1016/j.bmcl.2005.03.052

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  1 in total

1.  Optimization of biaryl piperidine and 4-amino-2-biarylurea MCH1 receptor antagonists using QSAR modeling, classification techniques and virtual screening.

Authors:  Georgia Melagraki; Antreas Afantitis; Haralambos Sarimveis; Panayiotis A Koutentis; John Markopoulos; Olga Igglessi-Markopoulou
Journal:  J Comput Aided Mol Des       Date:  2007-03-22       Impact factor: 4.179

  1 in total

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