Agents for the Treatment of Overactive Detrusor. IV.1)Synthesis and Structure-Activity Relationships of Cyclic Analogues of Terodiline

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 hydrochloride (42.HC1), (+ hydrochloride (-+-)-(43a • HC1), (—) hydrochloride (—)-(43a • HC1), and methanesulfonate (43b • MsOH) showed stronger inhibitory activity on detrusor contraction than terodiline. © 1993, The Pharmaceutical Society of Japan. All rights reserved.