Synthesis and antimuscarinic activity of some ether- and thioether-bearing 1,3-dioxolanes and related sulfoxides and sulfones

A series of 1,3-dioxolane-based ligands, bearing ether, thioether and related sulfoxide and sulfone functionalities, were synthesised and tested as potential muscarinic antagonists. The compounds display moderate to low affinity for the three receptor subtypes M 1–M 3, with some of them showing a si...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry 1998-06, Vol.6 (6), p.825-832
Main Authors: Malmusi, Luca, Franchini, Silvia, Mucci, Adele, Schenetti, Luisa, Gulini, Ugo, Marucci, Gabriella, Brasili, Livio
Format: Article
Language:English
Subjects:
Animals
Dioxolanes - chemical synthesis
Dioxolanes - chemistry
Dioxolanes - pharmacology
Guinea Pigs
Heart - drug effects
Ileum - drug effects
In Vitro Techniques
Male
Muscarinic Antagonists - chemical synthesis
Muscarinic Antagonists - chemistry
Muscarinic Antagonists - pharmacology
Rabbits
Receptor, Muscarinic M1
Receptor, Muscarinic M2
Receptor, Muscarinic M3
Receptors, Muscarinic - drug effects
Structure-Activity Relationship
Sulfones - chemical synthesis
Sulfones - chemistry
Sulfones - pharmacology
Sulfoxides - chemical synthesis
Sulfoxides - chemistry
Sulfoxides - pharmacology
Vas Deferens - drug effects
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Summary:A series of 1,3-dioxolane-based ligands, bearing ether, thioether and related sulfoxide and sulfone functionalities, were synthesised and tested as potential muscarinic antagonists. The compounds display moderate to low affinity for the three receptor subtypes M 1–M 3, with some of them showing a significant selectivity for the M 1–M 3 over the M 2 subtype.
ISSN:0968-0896
1464-3391
DOI:10.1016/S0968-0896(98)00042-X