Abstract
A series of novel aminobenzimidazoles was prepared and evaluated for h-MCH-R1 antagonist properties. Most of the compounds showed excellent h-MCH-R1 binding affinity as well as mouse ex vivo binding. Compounds 9 and 18 were active in mouse DIO studies at 30mpk.
MeSH terms
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Animals
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Anti-Obesity Agents / chemistry
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Anti-Obesity Agents / pharmacology*
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Benzimidazoles / chemistry
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Benzimidazoles / pharmacology*
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Benzimidazoles / therapeutic use*
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Binding, Competitive / drug effects
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Diet
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Disease Models, Animal
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Drug Evaluation, Preclinical
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Eating / drug effects
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Humans
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Metabolic Diseases / drug therapy*
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Mice
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Mice, Obese
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Molecular Conformation
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Obesity / drug therapy
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Rats
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Receptors, Somatostatin / antagonists & inhibitors*
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Stereoisomerism
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Structure-Activity Relationship
Substances
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Anti-Obesity Agents
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Benzimidazoles
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MCHR1 protein, human
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Receptors, Somatostatin