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2H-[1]benzothiepino [5,4-b]pyran derivatives with local anesthetic and antiarrhythmic activities.

作者信息

Longobardi M, Bargagna A, Mariani E, Schenone P, Vitagliano S, Stella L, Di Sarno A, Marmo E

机构信息

Istituto di Farmaceutiche dell'Università, Genova, Italy.

出版信息

Farmaco. 1990 Apr;45(4):399-404.

PMID:2400514
Abstract

The synthesis of some N,N-disubstituted 4-amino-5,6-dihydro-3-phenyl-2H-[1]benzothiepino [5,4-b]pyran-2-ones by reaction of phenylchloroketene with a series of N,N-disubstituted (E)-4-aminomethylene-3,4-dihydro-1-benzothiepin-5(2H)-ones, followed by dehydrochlorination of the primary adducts with DBN, is described. The 4-methylphenylamino derivative showed a local anesthetic activity in mice superior to that of lidocaine and the 4-morpholino derivative showed an antiarrhythmic activity in rats comparable to that of quinidine.

摘要

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