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Aminopyrazoles with high affinity for the human neuropeptide Y5 receptor
C P Kordik1, C Luo, B C Zanoni
1Drug Discovery Division, The R. W. Johnson Pharmaceutical Research Institute, Welsh and McKean Roads, Spring House, PA 19477, USA. ckordik@prius.jnj.com
Bioorganic & Medicinal Chemistry Letters
|August 31, 2001
Abstract:
1,3-Disubstituted-5-aminopyrazoles were prepared based on a lead compound found through high-throughput screening of our corporate compound library in an assay measuring affinity for the human neuropeptide Y5 receptor. The target compounds were prepared by cyclization of alpha-cyanoketones with appropriate hydrazines, followed by reduction and coupling to various sulfonamido-carboxylic acids. Several of these arylpyrazoles (e.g., 19 and 45) displayed high affinity for the human NPY Y5 receptor (<20nM IC(50)s).