Abstract
Optimization of a series of constrained melanin-concentrating hormone receptor 1 (MCH R1) antagonists has provided compounds with potent and selective MCH R1 activity. Details of the optimization process are provided and the use of one of the compounds in an animal model of diet-induced obesity is presented.
MeSH terms
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Animals
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Body Weight / drug effects
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Mice
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Mice, Inbred AKR
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Models, Molecular
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Molecular Structure
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Pyrimidinones / chemical synthesis
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Pyrimidinones / chemistry*
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Pyrimidinones / pharmacology*
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Receptors, Pituitary Hormone / antagonists & inhibitors*
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Receptors, Pituitary Hormone / metabolism
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Structure-Activity Relationship
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Sulfhydryl Compounds / chemistry
Substances
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Pyrimidinones
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Receptors, Pituitary Hormone
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Sulfhydryl Compounds
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melanin-concentrating hormone receptor