Agents for the Treatment of Overactive Detrusor. IV. Synthesis and Structure-Activity Relationships of Cyclic Analogues of Terodiline

…, K OKUMURA, K TSUBAKI, T TERAI…

Index: Take; Okumura; Tsubaki; Terai; Shiokawa Chemical and Pharmaceutical Bulletin, 1993 , vol. 41, # 3 p. 507 - 515

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Abstract

A series of pyrrolidine derivatives were synthesized and examined for inhibitory activity on detrusor contraction in vivo. Among those compounds, 5, 5-dimethyl-2 (2, 2-diphenylethyl)-3- isopropylidenepyrrolidine hydrochloride (41· HCl), 2-(2, 2-di (4-fluorophenyl) ethylene)-5, 5- dimethyl-3-isopropylidenepyrrolidine hydrochloride (42· HCl),(+)-5, 5-dimethyl-2-(N, N- diphenylaminomethyl)-3-isopropylidenepyrrolidine hydrochloride (+)-(43a· HCl),(-)-5, 5-di- ...