Abstract
Completing a long-lasting research on 1,3-oxathiolane muscarinic ligands, we have synthesized a set of isomeric 1-methyl-2-(2,2-alkylaryl-1,3-oxathiolan-5-yl)pyrrolidine 3-sulfoxide derivatives, containing three or four stereogenic centers. In general the compounds are very potent antagonists even if, unlike the corresponding agonists, they show modest subtype selectivity.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Binding Sites
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CHO Cells
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Cells, Cultured
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Cricetinae
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Cricetulus
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Dose-Response Relationship, Drug
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Guinea Pigs
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Ligands
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Male
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Models, Molecular
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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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Pyrrolidines / chemical synthesis*
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Pyrrolidines / chemistry
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Pyrrolidines / pharmacology*
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Rabbits
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Receptors, Muscarinic / drug effects
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Stereoisomerism
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Structure-Activity Relationship
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Sulfoxides / chemical synthesis*
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Sulfoxides / chemistry
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Sulfoxides / pharmacology*
Substances
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Ligands
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Muscarinic Antagonists
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Pyrrolidines
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Receptors, Muscarinic
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Sulfoxides