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Pyrazolecarboxamide human neuropeptide Y5 receptor ligands with in vivo antifeedant activity
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@pruis.jnj.com
Bioorganic & Medicinal Chemistry Letters
|August 31, 2001
Abstract:
1-Aryl-3-carboxamido-5-alkylpyrazoles were prepared based on a hit found in high-throughput screening of our corporate compound library in an assay measuring affinity for the human neuropeptide Y5 receptor. 1-(3-Trifluoromethylphenyl)-3-[N-(5-quinolinyl)carboxamido]-5-methylpyrazole (31) bound to the human neuropeptide Y5 receptor with a 80 nM IC(50 )and was shown to inhibit cumulative food consumption 43.2% 2-6 h after ip dosing in a fasting-induced feeding model in rats.