Abstract
The synthesis and biological evaluation of a novel family of M(3) muscarinic antagonists are described. A systematic modification of the substituents to a novel alkyne-quinuclidine scaffold yielded original compounds displaying potent in vitro anticholinergic properties.
MeSH terms
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Animals
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Binding Sites
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Cytochrome P-450 CYP2D6 Inhibitors
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Cytochrome P-450 CYP3A
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Cytochrome P-450 Enzyme Inhibitors
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Drug Evaluation, Preclinical
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Guinea Pigs
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Humans
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In Vitro Techniques
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Microsomes / drug effects
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Microsomes / enzymology
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Molecular Structure
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Muscarinic Antagonists / chemical synthesis
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Muscarinic Antagonists / chemistry
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Muscarinic Antagonists / pharmacology*
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Quinuclidines / chemical synthesis
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Quinuclidines / chemistry
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Quinuclidines / pharmacology*
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Receptors, Muscarinic / drug effects*
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Receptors, Muscarinic / metabolism
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Structure-Activity Relationship
Substances
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Cytochrome P-450 CYP2D6 Inhibitors
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Cytochrome P-450 Enzyme Inhibitors
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Muscarinic Antagonists
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Quinuclidines
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Receptors, Muscarinic
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CYP3A protein, human
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Cytochrome P-450 CYP3A