192323-20-9Relevant academic research and scientific papers
Design, synthesis and SAR of a series of 2-substituted 4-amino-quinazoline neuropeptide Y Y5 receptor antagonists
Rueeger, Heinrich,Rigollier, Pascal,Yamaguchi, Yasuchika,Schmidlin, Tibur,Schilling, Walter,Criscione, Leoluca,Whitebread, Steven,Chiesi, Michele,Walker, Mary W.,Dhanoa, Dale,Islam, Imadul,Zhang, Jack,Gluchowski, Charles
, p. 1175 - 1179 (2007/10/03)
The design of a novel series of NPY-Y5 receptor antagonists is described. Key elements for the design were the identification of weak Y5 hits from a Y1 program, results from a combinatorial approach and database mining. This led to the discovery of the quinazoline 4 and the aryl-sulphonamide moiety as major components of the pharmacophore for Y5 affinity. The synthesis and SAR towards CGP71683A is described. (C) 2000 Elsevier Science Ltd. All rights reserved.
