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PubMed · 31474

2-Methoxyphenylethanolamines, potential beta-adrenergic blocking agents.

L R Williams·B V Lap·C H Lim·D M Temple·P A Easson·G L Letts
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Abstract

The effect of the introduction of a 2-methoxy substituent on the beta-adrenergic antagonistic properties of a series of 3- and 4-substituted phenylethanolamines (1) was studied. Both the series of bromo- and methyl-substituted compounds behaved similarly, indicating that electronic forces are not significant in determining beta-adrenergic antagonist activity. When compared with the corresponding phenylethanolamines without a 2-methoxy substitutent, the 2-methoxy-4-substituted derivatives (3a and 3d) had enhanced potency and selectivity but the 2,3- (3b and 3e) and the 2,5-disubstitution patterns (3c and 3f) showed a loss of activity. The inconsistent changes in activity prevented any firm conclusions being made about the effect of the ether oxygen and the beta-adrenoceptor antagonistic activity of phenoxypropanolamines.

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Adrenergic beta-AntagonistsAnimalsEthanolaminesGuinea PigsHeartIn Vitro TechniquesIsoproterenolStructure-Activity RelationshipTracheaJournal Article

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L R Williams, B V Lap, C H Lim, D M Temple, P A Easson, G L Letts. 1978. 2-Methoxyphenylethanolamines, potential beta-adrenergic blocking agents.. https://doi.org/10.1021/jm00208a015

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