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Cycloocta[b]pyran derivatives with local anesthetic, platelet antiaggregating and other activities.

作者信息

Longobardi M, Bargagna A, Mariani E, Schenone P, D'Amico M, Falciani M, Filippelli W, Contaldi C

机构信息

Istituto di Farmacologia e Tossicologia, Facoltà di Medicina e Chirurgia, II Università degli studi di Napoli, Italy.

出版信息

Farmaco. 1995 Jan;50(1):55-9.

PMID:7702722
Abstract

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.

摘要

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