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Synthesis and antitussive activity of aminotetra- (and -hexa-) hydrodibenzofurans.

Abstract：

:The synthesis of a novel series of antitussive agents is described. Two series of amino-substituted tetra- and hexahydrodibenzofurans were prepared and examined for antitussive activity in the guinea pig after cough elicited by electrical stimulation of the vagus nerve. A significant level of activity, comparable with that of codeine, was found in the 4alpha-amino series. The 4-methylpiperazin-1-ylpropionamide (28) was found to be the most active of the compounds synthesized and was equipment with codeine. The effects of structural modification upon antitussive activity were investigated in numerous analogues but no enhancement of activity was achieved over that of 28.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Matharu SS,Rowlands DA,Taylor JB,Westwood R

doi

10.1021/jm00212a003

subject

Has Abstract

pub_date

1977-02-01 00:00:00

pages

197-204

issue

2

eissn

0022-2623

issn

1520-4804

journal_volume

20

pub_type

杂志文章

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