192323-01-6Relevant academic research and scientific papers
Discovery of potent and selective small molecule NPY Y5 receptor antagonists.
Islam, Imadul,Dhanoa, Dale,Finn, John,Du, Ping,Walker, Mary W,Salon, John A,Zhang, Jack,Gluchowski, Charles
, p. 1767 - 1769 (2007/10/03)
The discovery of a new class of sulfonamide NPY Y5 receptor antagonists is described. Optimization of this series led to the identification of compounds with high affinity for the hY5 subtype and excellent selectivity over the other NPY receptor subtypes. The SAR for this series was examined and a model for understanding the ligand-receptor interactions was developed.
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.
