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1. Synthesis and evaluation of new arylsulfonamidomethylcyclohexyl derivatives as human neuropeptide Y Y5 receptor antagonists for the treatment of obesity.

Author

Moreno A, Pérez S, Galiano S, Juanenea L, Erviti O, Frígola C, Aldana I, and Monge A

Subjects
Animals, Binding, Competitive drug effects, Cell Line, Drug Evaluation, Preclinical, Humans, Molecular Structure, Obesity drug therapy, Structure-Activity Relationship, Anti-Obesity Agents pharmacology, Cyclohexanes chemical synthesis, Cyclohexanes pharmacology, Receptors, Neuropeptide Y antagonists & inhibitors, Sulfonamides chemical synthesis, Sulfonamides pharmacology
Abstract

NPY is the most potent orexigenic peptide identified up to now. Stimulation of food intake is measured by the Y(1) and Y(5) receptor subtypes. In this study, the synthesis and evaluation of new arylsulfonamidomethylcyclohexyl derivatives are described as potential selective antagonists of the human NPY Y(5) receptor. The SAR of these series was examined and the amide derivatives were the compounds that showed the best activities. trans-N-(4-[(Quinolin-3-yl)aminocarbonyl]cyclohexylmethyl)-2,4-dichlorobenzenesulfonamide (42) bound to the human neuropeptide Y Y(5) receptor with a 2 nM IC(50).

Published
2004
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