Synthesis and Biological Activity of 11-[4-(Cinnamyl)-1-piperazinyl]-6, 11-dihydrodibenz[b, e]oxepin Derivatives, Potential Agents for the Treatment of Cerebrovascular Disorders

Mikio KUROKAWA; Fuminori SATO; Yoshinobu MASUDA; Takayuki YOSHIDA; Yuko OCHI; Kayoko ZUSHI; Iwao FUJIWARA; Shunsuke NARUTO; Hitoshi UNO; Jun-ichi MATSUMOTO

doi:10.1248/cpb.39.2564

Mikio KUROKAWA, Fuminori SATO, Yoshinobu MASUDA, Takayuki YOSHIDA, Yuko OCHI, Kayoko ZUSHI, Iwao FUJIWARA, Shunsuke NARUTO, Hitoshi UNO, Jun-ichi MATSUMOTO

Author information

Mikio KUROKAWA
Fuminori SATO
Yoshinobu MASUDA
Takayuki YOSHIDA
Yuko OCHI
Kayoko ZUSHI
Iwao FUJIWARA
Shunsuke NARUTO
Hitoshi UNO
Jun-ichi MATSUMOTO
Author's Organization：
Research Laboratories, Dainippon Pharmaceutical Co., Ltd.,
Research Laboratories, Dainippon Pharmaceutical Co., Ltd.,
Research Laboratories, Dainippon Pharmaceutical Co., Ltd.,
Research Laboratories, Dainippon Pharmaceutical Co., Ltd.,
Research Laboratories, Dainippon Pharmaceutical Co., Ltd.,
Research Laboratories, Dainippon Pharmaceutical Co., Ltd.,
Research Laboratories, Dainippon Pharmaceutical Co., Ltd.,
Research Laboratories, Dainippon Pharmaceutical Co., Ltd.,
Research Laboratories, Dainippon Pharmaceutical Co., Ltd.,
Research Laboratories, Dainippon Pharmaceutical Co., Ltd.,

Keywords: cerebrovascular disorder, anti-ischemic effect, antihypoxic effect, anti-lipidperoxidation, anticonvulsion, anti-cerebral edema, 11-[4-(cinnamyl)-1-piperaziny]-6, 11-dihydrodibenz[b, e]oxepin, structure-activity relationship

JOURNAL FREE ACCESS

1991 Volume 39 Issue 10 Pages 2564-2573

DOI https://doi.org/10.1248/cpb.39.2564

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Abstract

A series of 11-[4-(cinnamyl)-1-piperazinyl]-6, 11-dihydrodibenz[b, e]oxepins and related compounds were synthesized and evaluated for their protective activities against complete ischemia, normobaric hypoxia, lipidperoxidation and convulsion. Structure-activity relationship studies of this series led to the finding of (E)-1-(3-fluoro-6, 11-dihydrodibenz[b, e]oxepin-11-yl)-4-(3-phenyl-2-propenyl)piperazine dimaleate (50), AJ-3941 with the most appropriate property for combined pharmacological activities.

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