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Synthesis and Antimuscarinic Activity of Derivatives of 2-Substituted-1,3-Dioxolanes
Authors:Gabriella Marucci  Angeli Piero  Livio Brasili  Michela Buccioni  Dario Giardinà  Ugo Gulini  Alessandro Piergentili  Gianni Sagratini
Affiliation:(1) Department of Chemical Sciences, University of Camerino, Via S. Agostino 1, Camerino (MC), Italy, I-62032;(2) Department of Pharmaceutical Sciences, University of Modena and Reggio Emilia, Via Campi 183, Modena, Italy, I-41100
Abstract:
Geometric cis, trans isomers, derivatives of 2-substituted-1,3-dioxanes were designed and studied as antimuscarinic agents. The synthesized compounds were evaluated as perchlorides and methiodides by functional tests with rabbit vas deferens (putative M1), guinea-pig heart (M2) and guinea-pig ileum (M3). The effect of the replacement of a trimethylammonium group with a dimethysulfonium in the two rings was also evaluated. Pharmacological results indicate that the 1,3-dioxane nucleus shows the highest stereoselective values on the studied receptors.
Keywords:
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