Agents for the treatment of overactive detrusor. IX. Synthesis and pharmacological properties of metabolites of N-tert-Butyl-4, 4-diphenyl-2-cyclopentenylamine (FK584 …

…, Y Miyao, K Yamano, T YAMAMOTO, T Terai…

Index: Taniguchi, Kiyoshi; Miyao, Yasuhiro; Yamano, Katsuhiro; Yamamoto, Takao; Terai, Takao; Kusunoki, Takahiro; Tsubaki, Kazunori; Shiokawa, Youichi Chemical and Pharmaceutical Bulletin, 1996 , vol. 44, # 6 p. 1188 - 1195

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Abstract

We synthesized the racemates of five presumed metabolites (1b-f) of (S)-(-)-N-tert-butyl-4, 4- diphenyl-2-cyclopentenylamine hydrochloride (FK584, S (-)-1a), a novel agent for the treatment of overactive detrusor syndrome, in order to confirm the structures of the metabolites and also to evaluate thier inhibitory activity against detrusor contraction.(±)-N- tert-Butyl-4-(4-hydroxyphenyl)-and 4-(4-hydroxy-3-methoxyphenyl)-4-phenyl-2- ...