Aminopyrazoles with high affinity for the human neuropeptide Y5 receptor

1,3-Disubstituted-5-aminopyrazoles were prepared based on a lead compound f ound through high-throughput screening of our corporate compound library in an assay measuring affinity for the human neuropeptide Y5 receptor. The ta rget compounds were prepared by cyclization of alpha -cyanoketones with app ropriate hydrazines, followed by reduction and coupling to various sulfonam ido-carboxylic acids. Several of these arylpyrazoles (e.g., 19 and 45) disp layed high affinity for the human NPY Y5 receptor (< 20 nM IC(50)s). (C) 20 01 Elsevier Science Ltd. All rights reserved.