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, G; Angeli, P; Brasili, Livio; Buccioni, M; Giardinà, D; Gulini, U; Piergentili, A; Sagratini, G; Franchini, Silvia. - In: MEDICINAL CHEMISTRY RESEARCH. - ISSN 1054-2523. - STAMPA. - 14:(2005), pp. 309-331. [10.1007/s00044-006-0143-5]
Synthesis and antimuscarinic activity of derivatives of 2-substituted-1,3-dioxolanes
BRASILI, Livio;FRANCHINI, Silvia
2005
Abstract
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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