Abstract
A series of cyclohexylpiperazines was synthesized as potent and selective antagonists of the human MC4 receptor. Compound 14t displayed binding affinity (Ki) of 4.2 and 1100 nM at MC4R and MC3R, respectively.
MeSH terms
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Amides / chemistry*
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Binding, Competitive
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Humans
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Molecular Conformation
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Piperidines / chemical synthesis
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Piperidines / chemistry
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Piperidines / pharmacology*
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Receptor, Melanocortin, Type 3 / antagonists & inhibitors
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Receptor, Melanocortin, Type 4 / antagonists & inhibitors*
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Structure-Activity Relationship
Substances
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Amides
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MC4R protein, human
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Piperidines
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Receptor, Melanocortin, Type 3
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Receptor, Melanocortin, Type 4