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.

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. Compound 50 also shows an inhibitory effect against cerebral edema as well when orally given to rats.
Authors	M Kurokawa, F Sato, Y Masuda, T Yoshida, Y Ochi, K Zushi, I Fujiwara, S Naruto, H Uno, J Matsumoto
Journal	Chemical & pharmaceutical bulletin (Chem Pharm Bull (Tokyo)) Vol. 39 Issue 10 Pg. 2564-73 (Oct 1991) ISSN: 0009-2363 [Print] Japan
PMID	1806275 (Publication Type: Journal Article)
Chemical References	Benzothiepins Benzoxepins Piperazines Flunarizine
Topics	Animals Benzothiepins (chemical synthesis, pharmacology, therapeutic use) Benzoxepins (chemical synthesis, pharmacology, therapeutic use) Brain Edema (drug therapy) Brain Ischemia (drug therapy) Cerebrovascular Disorders (drug therapy) Flunarizine (pharmacology, therapeutic use) Hypoxia, Brain (drug therapy) Mice Piperazines (chemical synthesis, pharmacology, therapeutic use) Rats Structure-Activity Relationship

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