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ID: ALA1132894
Journal: Bioorg Med Chem Lett
Title: Design, synthesis and SAR of a series of 2-substituted 4-amino-quinazoline neuropeptide Y Y5 receptor antagonists.
Authors: Rueeger H, Rigollier P, Yamaguchi Y, Schmidlin T, Schilling W, Criscione L, Whitebread S, Chiesi M, Walker MW, Dhanoa D, Islam I, Zhang J, Gluchowski C.
Abstract: 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.
CiteXplore: 10866375