心脏选择性β-肾上腺素能阻滞剂。1. 1-((3,4-二甲氧基苯乙基)氨基)-3 - 芳氧基-2-丙醇。
Cardioselective beta-adrenergic blocking agents. 1. 1-((3,4-Dimethoxyphenethyl)amino)-3-aryloxy-2-propanols.
作者信息
Hoefle M L, Hastings S G, Meyer R F, Corey R M, Holmes A, Stratton C D
出版信息
J Med Chem. 1975 Feb;18(2):148-52. doi: 10.1021/jm00236a007.
PMID:235644
Abstract
A series of 1-amino-3-aryloxy-2-propanols has been synthesized and examined for cardioselective beta-blockade. The introduction of the (3,4-dimethoxyphenethyl)amino group lead to the most cardioselective agents. Structure-activity relationships are discussed. Of the compounds tested 1-[(3,4-dimethoxyphenethyl)amino]-3-(m-tolyloxy)-2-propanol was selected for clinical trial because of optimal potency and selectivity.
摘要
已合成了一系列1-氨基-3-芳氧基-2-丙醇，并对其进行了心脏选择性β受体阻滞作用的研究。引入(3,4-二甲氧基苯乙基)氨基得到了最具心脏选择性的药物。讨论了构效关系。在所测试的化合物中，1-[(3,4-二甲氧基苯乙基)氨基]-3-(间甲苯氧基)-2-丙醇因其最佳的效力和选择性而被选作临床试验药物。
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