2-甲氧基苯乙醇胺，潜在的β-肾上腺素能阻滞剂。

2-Methoxyphenylethanolamines, potential beta-adrenergic blocking agents.

作者信息

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

出版信息

J Med Chem. 1978 Oct;21(10):1081-4. doi: 10.1021/jm00208a015.

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.

摘要

研究了引入2-甲氧基取代基对一系列3-和4-取代苯乙醇胺（1）的β-肾上腺素能拮抗特性的影响。溴代和甲基取代的化合物系列表现相似，表明电子作用力在决定β-肾上腺素能拮抗剂活性方面并不显著。与没有2-甲氧基取代基的相应苯乙醇胺相比，2-甲氧基-4-取代衍生物（3a和3d）的效力和选择性增强，但2,3-（3b和3e）和2,5-二取代模式（3c和3f）显示活性丧失。活性的不一致变化使得无法就醚氧的作用和苯氧丙醇胺的β-肾上腺素能受体拮抗活性得出任何确凿结论。