Abstract
Novel derivatives of Tolterodine (1) and Oxybutynin (2) have been designed using conformationally restricted azabicyclics as replacement for open-chain amines. The synthesis and structure-activity relationships are presented.
MeSH terms
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Animals
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Benzhydryl Compounds / chemical synthesis*
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Benzhydryl Compounds / metabolism
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Benzhydryl Compounds / pharmacology*
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Binding Sites / drug effects
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Cresols / chemical synthesis*
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Cresols / metabolism
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Cresols / pharmacology*
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Drug Design*
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Mandelic Acids / chemical synthesis*
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Mandelic Acids / metabolism
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Mandelic Acids / pharmacology*
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Phenylpropanolamine / chemical synthesis*
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Phenylpropanolamine / metabolism
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Phenylpropanolamine / pharmacology*
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Rats
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Receptor, Muscarinic M2 / metabolism
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Receptor, Muscarinic M3 / metabolism
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Structure-Activity Relationship
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Tolterodine Tartrate
Substances
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Benzhydryl Compounds
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Cresols
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Mandelic Acids
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Receptor, Muscarinic M2
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Receptor, Muscarinic M3
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Phenylpropanolamine
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Tolterodine Tartrate
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oxybutynin