Abstract
Spiroindoline urea derivatives, designed to act as NPY Y5 receptor antagonists, were synthesized and their structure-activity relationships were investigated. Of these derivatives, compound 3a showed good Y5 binding affinity with favorable pharmacokinetic properties. Compound 3a significantly inhibited bPP Y5 agonist-induced food intake in rats, and suppressed body weight gain in DIO mice.
MeSH terms
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Animals
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Anti-Obesity Agents / chemical synthesis
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Anti-Obesity Agents / chemistry*
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Anti-Obesity Agents / pharmacokinetics
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Anti-Obesity Agents / pharmacology*
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Biological Availability
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Body Weight / drug effects
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Eating / drug effects
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Indoles / chemical synthesis
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Indoles / chemistry*
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Indoles / pharmacokinetics
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Indoles / pharmacology*
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Mice
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Mice, Inbred C57BL
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Molecular Structure
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Protein Binding
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Rats
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Rats, Sprague-Dawley
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Receptors, Neuropeptide Y / agonists
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Receptors, Neuropeptide Y / antagonists & inhibitors*
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Receptors, Neuropeptide Y / metabolism*
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Spiro Compounds / chemical synthesis
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Spiro Compounds / chemistry
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Spiro Compounds / pharmacokinetics
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Spiro Compounds / pharmacology
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Structure-Activity Relationship
Substances
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Anti-Obesity Agents
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Indoles
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Receptors, Neuropeptide Y
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Spiro Compounds
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neuropeptide Y5 receptor
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indoline