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
- 作者：Silvia Dei ; Cristina Bellucci ; Michela Buccioni ; Marta Ferraroni ; Luca Gu ; alini ; Dina Manetti ; Gabriella Marucci ; Rosanna Matucci ; Marta Nesi ; Maria Novella Romanelli ; Serena Scapecchi ; Elisabetta Teo
- 关键词：Muscarinic antagonists ; Affinity ; Functional activity ; 1 ; 3-Oxathiolane sulfoxides
- 刊名：Bioorganic and Medicinal Chemistry
- 出版年：2008
- 期刊代码：9_09680896
- 类别：ch
- 出版时间：15 May 2008
- 卷：16
- 期：10
- 页码：5490-5500
- 文件大小：283 K
摘要
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.