Abstract
A novel series of benzimidazoles was identified and optimized, leading to the discovery of potent and selective antagonists of the human melanocortin-4 receptor. In addition, compound 5i was shown to cross the blood-brain barrier after intravenous dosing in rats.
MeSH terms
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Animals
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Area Under Curve
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Benzimidazoles / blood
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Benzimidazoles / chemistry*
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Benzimidazoles / pharmacology*
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Blood-Brain Barrier
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Brain / metabolism
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Half-Life
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Humans
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Molecular Structure
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Rats
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Receptor, Melanocortin, Type 4 / antagonists & inhibitors*
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Structure-Activity Relationship
Substances
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Benzimidazoles
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Receptor, Melanocortin, Type 4