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

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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 4.alpha.-amino series. The 4-methylpiperazin-1-ylpropionamide (28) was the most active of the compounds synthesized and was equipotent with codeine. The effects of structural modification on antitussive activity were investigated in numerous analogues but no enhancement of activity was achieved over that of 28.

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