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2 results on '"Juanenea L"'

1. New amide derivatives as melanin-concentrating hormone receptor 1 antagonists for the treatment of obesity.

Author

Cirauqui N, Ceras J, Galiano S, Pérez-Silanes S, Juanenea L, Rivera G, Aldana I, and Monge A

Subjects
Animals, CHO Cells, Cricetinae, Cricetulus, Humans, Indicators and Reagents, Solvents, Structure-Activity Relationship, Amides chemical synthesis, Amides pharmacology, Anti-Obesity Agents chemical synthesis, Anti-Obesity Agents pharmacology, Receptors, Somatostatin antagonists & inhibitors
Abstract

Melanin-concentrating hormone (MCH) is a recently discovered central nervous system (CNS) target for treating obesity. Two novel series of amide derivatives were synthesized and evaluated biologically as MCH-R1 (melanin-concentrating hormone receptor 1) antagonists. The results showed that diphenyl substituents on the amide lead to better activity than biphenyl substituents.

Published
2008
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2. Novel human neuropeptide Y Y5 receptor antagonists for the treatment of obesity. Synthesis and biological evaluation of pyridine hydrazide derivatives.

Author

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

Subjects
Humans, Indicators and Reagents, Stereoisomerism, Structure-Activity Relationship, Sulfonamides chemical synthesis, Anti-Obesity Agents chemical synthesis, Anti-Obesity Agents therapeutic use, Hydrazines chemical synthesis, Hydrazines therapeutic use, Obesity drug therapy, Pyridines chemical synthesis, Pyridines therapeutic use, Receptors, Neuropeptide Y antagonists & inhibitors
Abstract

A series of new pyridine hydrazide derivatives with high and selective antagonist activity at the human neuropeptide Y Y5 receptor were developed. Introduction of electron-withdrawing groups into the arylsulfonamide rest, together with the 3-pyridyl analogue in the hydrazide moiety, led to a significant improvement of potency and solubility, affording trans-N-(4-[N'-(pyridine-3-carbonyl)hydrazino-carbonyl]cyclohexylmethyl)-2,4-dichloro-benzenesulfonamide (14), which binds to the hY5 receptor with an IC50 value of 7.44 nmol/L.

Published
2005
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