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, 16 (10), 5490-500

Muscarinic Antagonists With Multiple Stereocenters: Synthesis, Affinity Profile and Functional Activity of Isomeric 1-methyl-2-(2,2-alkylaryl-1,3-oxathiolan-5-yl)pyrrolidine Sulfoxide Derivatives

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Muscarinic Antagonists With Multiple Stereocenters: Synthesis, Affinity Profile and Functional Activity of Isomeric 1-methyl-2-(2,2-alkylaryl-1,3-oxathiolan-5-yl)pyrrolidine Sulfoxide Derivatives

Silvia Dei et al. Bioorg Med Chem.

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.

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