Abstract
High-throughput screening revealed diaryl pyrazole 3 as a selective albeit modest cholecystokinin 1 receptor (CCK1R) agonist. SAR studies led to the discovery and optimization of a novel class of 1,2-diaryl imidazole carboxamides. Compound 44, which was profiled extensively, showed good in vivo mouse gallbladder emptying (mGBE) and lean mouse overnight food intake (ONFI) reduction activities.
MeSH terms
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Amides / chemical synthesis*
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Amides / chemistry
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Amides / pharmacology*
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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 / pharmacology*
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Chemokines, CC
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Combinatorial Chemistry Techniques
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Eating / drug effects
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Gallbladder Emptying / drug effects
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Humans
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Imidazoles / chemical synthesis*
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Imidazoles / chemistry
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Imidazoles / pharmacology*
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Mice
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Molecular Structure
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Receptors, Cholecystokinin / agonists*
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Structure-Activity Relationship
Substances
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Amides
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Anti-Obesity Agents
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Ccl28 protein, mouse
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Chemokines, CC
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Imidazoles
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Receptors, Cholecystokinin