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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Anti-Obesity Agents / chemical synthesis*
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Anti-Obesity Agents / therapeutic use*
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Humans
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Hydrazines / chemical synthesis*
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Hydrazines / therapeutic use*
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Indicators and Reagents
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Obesity / drug therapy*
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Pyridines / chemical synthesis*
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Pyridines / therapeutic use*
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Receptors, Neuropeptide Y / antagonists & inhibitors*
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Stereoisomerism
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Structure-Activity Relationship
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Sulfonamides / chemical synthesis
Substances
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Anti-Obesity Agents
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Hydrazines
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Indicators and Reagents
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Pyridines
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Receptors, Neuropeptide Y
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Sulfonamides
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neuropeptide Y5 receptor