H. Tucker
Oct 1, 1980
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0
Influential Citations
5
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Quality indicators
Journal
Journal of medicinal chemistry
Abstract
The synthesis of a series of (3-hydroxyprop-1-enyl)-substituted 1-(aryloxy)-3-(alkylamino)propan-2-ols is described. These compounds were investigated for their beta-adrenoreceptor blocking properties and their selective of action. Among the o-(hydroxypropenyl)-substituted derivatives we have found some potent noncardioselective beta-adrenoreceptor blocking agents which have a greater blocking action on the beta 2 receptor, thus resembling propranolol. The p-(hydroxypropenyl)-substituted analogues were generally less potent and tended to be cardioselective. The structure-activity relationships are discussed in the light of the hypothesis that the cardioselective of p-amido-substituted (aryloxy)propanolamines is attributable, in part, to binding of the amide group to some additional site on the beta receptor; our findings argue against a similar interaction for the allylic hydroxyl group.