Pyrazolecarboxamide Human Neuropeptide Y5 Receptor Ligands with in Vivo Antifeedant Activity
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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.
Adipose Y5R mRNA is higher in obese than non-obese humans and is correlated with obesity parameters.
Chatree S, Sitticharoon C, Maikaew P, Uawithya P, Chearskul S Exp Biol Med (Maywood). 2018; 243(9):786-795.
PMID: 29763369 PMC: 5956667. DOI: 10.1177/1535370218774889.
Hasaninejad A, Firoozi S Mol Divers. 2013; 17(3):459-69.
PMID: 23624645 DOI: 10.1007/s11030-013-9445-y.
Approaches towards the synthesis of 5-aminopyrazoles.
Aggarwal R, Kumar V, Kumar R, Singh S Beilstein J Org Chem. 2011; 7:179-97.
PMID: 21448263 PMC: 3063075. DOI: 10.3762/bjoc.7.25.