Abstract
A series of 4-substituted anilides with human melatonergic affinity is reported. Butyramides 26, 39, 42, 52, 57, and 58 all demonstrated subnanomolar MT(2) binding affinity and MT(2) selectivity of at least 70-fold over the MT(1) receptor. Compound 26 demonstrated full agonism at the MT(2) receptor.
MeSH terms
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Anilides / chemical synthesis
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Anilides / chemistry*
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Binding, Competitive
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Humans
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Melatonin / metabolism
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Molecular Structure
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Receptor, Melatonin, MT2 / agonists*
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Receptor, Melatonin, MT2 / chemistry
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Structure-Activity Relationship
Substances
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Anilides
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Receptor, Melatonin, MT2
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Melatonin