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

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 le...

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Veröffentlicht in:	Chemical & pharmaceutical bulletin 1991/10/25, Vol.39(10), pp.2564-2573
Hauptverfasser:	KUROKAWA, Mikio, SATO, Fuminori, MASUDA, Yoshinobu, YOSHIDA, Takayuki, OCHI, Yuko, ZUSHI, Kayoko, FUJIWARA, Iwao, NARUTO, Shunsuke, UNO, Hitoshi, MATSUMOTO, Jun-ichi
Format:	Artikel
Sprache:	eng
Schlagworte:	11-[4-(cinnamyl)-1-piperaziny]-6, 11-dihydrodibenz[b, e]oxepin Animals anti-cerebral edema anti-ischemic effect anti-lipidperoxidation anticonvulsion antihypoxic effect Benzothiepins - chemical synthesis Benzothiepins - pharmacology Benzothiepins - therapeutic use Benzoxepins - chemical synthesis Benzoxepins - pharmacology Benzoxepins - therapeutic use Brain Edema - drug therapy Brain Ischemia - drug therapy cerebrovascular disorder Cerebrovascular Disorders - drug therapy Chemistry Exact sciences and technology Flunarizine - pharmacology Flunarizine - therapeutic use Heterocyclic compounds Heterocyclic compounds with n hetero atom and also o and/or s, se, te hetero atoms Hypoxia, Brain - drug therapy Mice Organic chemistry Piperazines - chemical synthesis Piperazines - pharmacology Piperazines - therapeutic use Preparations and properties Rats Structure-Activity Relationship
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Zusammenfassung:	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.
ISSN:	0009-2363 1347-5223
DOI:	10.1248/cpb.39.2564