Geometric cis, trans isomers, derivatives of 2-substituted-1,3-dioxolanes and 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 rabit vas deferens (putatvie M1), guinea-pig heart (M2) and guinea-pig ileum (M3). The effect of the replacement of a trimethylammonium group with a dimethylsulfonium in the two rings was also evalutated. Pharmacological results indicate that the 1,3-dioxane nucleus shows the highest stereoselective values on the studied receptors

Geometric cis, traits isomers, derivatives of 2-substituted-1,3-dioxolanes and 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 M-1), guinea-pig heart (M-2) and guinea-pig ileum (M-3). The effect of the replacement of a trimethylammonium group with a dimethylsulfonium 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.

Synthesis and antimuscarinic activity of derivatives of 2-substituted-1,3-dioxolanes

MARUCCI, Gabriella;ANGELI, Piero;GIARDINA', Dario;PIERGENTILI, Alessandro;SAGRATINI, Gianni;
2005

Abstract

Geometric cis, trans isomers, derivatives of 2-substituted-1,3-dioxolanes and 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 rabit vas deferens (putatvie M1), guinea-pig heart (M2) and guinea-pig ileum (M3). The effect of the replacement of a trimethylammonium group with a dimethylsulfonium in the two rings was also evalutated. Pharmacological results indicate that the 1,3-dioxane nucleus shows the highest stereoselective values on the studied receptors
Geometric cis, traits isomers, derivatives of 2-substituted-1,3-dioxolanes and 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 M-1), guinea-pig heart (M-2) and guinea-pig ileum (M-3). The effect of the replacement of a trimethylammonium group with a dimethylsulfonium 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.
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11581/113058
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