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[Compounds with psychotropic activity. VIII. Synthesis and sedative activity of various 9-substituted derivatives of 5-phenylpyrrolo[2,1-d][1,5] benzothiazepine and cis-4,5-dihydro-4-hydroxy-5-phenylpyrrolo[2,1-d][1,5]benzothiazepine].

作者信息

Nacci V, Fiorini I, Vomero S, Taddei I, Taddei E

出版信息

Farmaco Sci. 1984 Apr;39(4):289-304.

PMID:6723946
Abstract

Syntheses of 9-chloro-, 9-trifluoromethyl- and 9-methoxy-5- phenylpyrrolo [2,1-d] [1,5] benzothiazepine [II a-c] and of cis-9-chloro- and cis-9-trifluoromethyl-4,5-dihydro-4-hydroxy-5- phenylpyrrolo [2,1-d] [1,5] benzothiazepine with the respective acetyl derivatives (III a-d), according to previously restated routes, are described. The sedative activity was tested against the anti-amphetamine activity in the rat. The 1-[5-trifluoromethyl-2-(alpha- hydroxycarbonylbenzyl ) thiophenyl + ++]-pyrrole ( NF34 ) and the pyrrolo [2,1-d] [1,5] benzothiazepine -5-carboxamide ( NF44 ) showed sedative activity similar to that of diazepam.

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