REACTION OF KETENES WITH N,N-DISUBSTITUTED ALPHA-AMINOMETHYLENEKETONES .28. CYCLOOCTA[B]PYRAN DERIVATIVES WITH LOCAL-ANESTHETIC, PLATELET ANTIAGGREGATING AND OTHER ACTIVITIES

被引:0
|
作者
LONGOBARDI, M [1 ]
BARGAGNA, A [1 ]
MARIANI, E [1 ]
SCHENONE, P [1 ]
DAMICO, M [1 ]
FALCIANI, M [1 ]
FILIPPELLI, W [1 ]
CONTALDI, C [1 ]
机构
[1] UNIV NAPLES 2,FAC MED & CHIRURG,IST FARMACOL & TOSSICOL,I-80138 NAPLES,ITALY
来源
FARMACO | 1995年 / 50卷 / 01期
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中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The synthesis of some N,N-disubstituted 4-amino-5,6,7,8,9,10-hexahydro-3-phenyl-2H-cycloocta[b]pyran-2-ones by reaction of phenylchloroketene with a series of N,N-disubstituted 2-aminomethylenecyclooctanones , followed by dehydrochlorination in situ of the primary adducts with DBN, is described. The dimethylamino derivative showed a local anesthetic activity in mice superior to that of lidocaine, and some compounds exhibited a platelet antiaggregating activity in vitro superior or comparable to that of acetylsalicylic acid, as well as weak antiarrhythmic and antiinflammatory activities in rats.
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页码:55 / 59
页数:5
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