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

Marucci, Gabriella; Angeli, Piero; Brasili, L.; Giardina', Dario; Gulini, U.; Piergentili, Alessandro; Sagratini, Gianni; Franchini, S.

doi:10.1007/s00044-006-0143-5

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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.

Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/11581/113058

Titolo:	Synthesis and antimuscarinic activity of derivatives of 2-substituted-1,3-dioxolanes
Autori:	MARUCCI, Gabriella ANGELI, Piero BRASILI L. GIARDINA', Dario GULINI U. PIERGENTILI, Alessandro SAGRATINI, Gianni FRANCHINI S. mostra contributor esterni nascondi contributor esterni
Data di pubblicazione:	2005
Rivista:	MEDICINAL CHEMISTRY RESEARCH
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
Handle:	http://hdl.handle.net/11581/113058
Appare nelle tipologie:	Articolo

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