Abstract
We have investigated phenol replacements in a series of diaryl amino piperidine delta opioid agonists. From this study we have demonstrated that the hydroxy functional group can be replaced with a primary amide group, giving enhanced activity at the delta receptor, increased selectivity versus mu and kappa as well as improved in vitro metabolic stability.
MeSH terms
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Analgesics / chemical synthesis
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Analgesics / chemistry*
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Analgesics / pharmacology
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Animals
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Diphenylamine / analogs & derivatives*
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Diphenylamine / chemical synthesis
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Diphenylamine / chemistry
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Diphenylamine / pharmacology
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Humans
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Microsomes, Liver / metabolism
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Piperidines / chemical synthesis
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Piperidines / chemistry*
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Piperidines / pharmacology
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Rats
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Receptors, Opioid, delta / agonists*
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Receptors, Opioid, delta / metabolism
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Structure-Activity Relationship
Substances
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Analgesics
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Piperidines
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Receptors, Opioid, delta
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piperidine
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Diphenylamine