Structure-activity relations for anticholinergic dioxolans

Abstract

4-Dimethylaminomethyl 1, 3-dioxolan derivatives have been examined for anticholinergic potency. Quaternary derivatives in which C-2 was substituted with two bulky substituents were found to have anticholinergic potencies similar to those of atropine in the peripheral nervous system. A comparison of the enantiomeric cis and trans 2-cyclohexyl-2-phenyl-4-dimethylaminomethyl-1, 3-dioxolan methiodides showed that the observed configurational selectivity depended mainly on the configuration at C-2 and not on the geometrical relation between C-2 and C-4.