Pyrazolecarboxamide human neuropeptide Y5 receptor ligands with in vivo antifeedant activity

Authors
Kordik, CP Luo, C Zanoni, BC Lovenberg, TW Wilson, SJ Vaidya, AH Crooke, JJ Rosenthal, DI Reitz, AB
Citation
Cp. Kordik et al., Pyrazolecarboxamide human neuropeptide Y5 receptor ligands with in vivo antifeedant activity, BIOORG MED, 11(17), 2001, pp. 2287-2290
Citations number
24
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
17
Year of publication
2001
Pages
2287 - 2290
Database
ISI
SICI code
0960-894X(20010903)11:17<2287:PHNYRL>2.0.ZU;2-#
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 me asuring affinity for the human neuropeptide Y5 receptor. 1-(3-Trifluorometh ylphenyl)-3-[N-(5-quinolinyl)carboxamido]-5-methylpyrazole (31) bound to th e human neuropeptide Y5 receptor with a 80 nM IC50 and was shown to inhibit cumulative food consumption 43.2% 2-6 It after ip dosing in a fasting-indu ced feeding model in rats. (C) 2001 Elsevier Science Ltd. All rights reserv ed.