Abstract
As a part of studies on antispasmodics, the structure-activity relationship was examined in N-alkyl diarylmethylenequinolizidinium bromides and N-alkyl diarylmethyleneindolizidinium bromides (6-33), which can be classified in to γ-substituted piperidine, β-substituted piperidine and β-substituted pyrrolidine. Compounds (6-33) exhibited potent anticholinergic activity due to having conformationally rigid bicyclic hetero rings compared to monocyclic antispasmodics such as diphemanil methylsulfate (1), timepidium bromide (2), prifinium bromide (4) and their unmodified compounds (3 and 5). Several compounds among them exhibited potent anticholinergic activity greater than that of atropine.
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