Synthesis and adrenolytic activity of 1-(1H-indol-4-yloxy)-3-{[2-(2-methoxyphenoxy)ethyl]amino}propan-2-ol and its enantiomers. Part 1

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• 作者：Graż ; yna Groszek ; Marek Bednarski ; Mał ; gorzata Dybał ; a ; Barbara Filipek
• 关键词：α ; ₁- ; α ; ₂- ; β ; ₁-Adrenoceptor antagonist ; Antiarrhythmic ; hypotensive and spasmolytic activities ; Synthesis
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2009
• 出版时间：February 2009
• 年：2009
• 卷：44
• 期：2
• 页码：809-817
• 全文大小：500 K

文摘

The synthesis of (2RS)-1-(1H-indol-4-yloxy)-3-{[2-(2-methoxyphenoxy)ethyl]amino}propan-2-ol ((RS)-9) and its enantiomers has been described and tested for electrocardiographic, antiarrhythmic, hypotensive and spasmolytic activities as well as for α₁-, α₂- and β₁-adrenoceptors' binding affinities. All compounds significantly decrease systolic and diastolic blood pressure, and possess antiarrhythmic activity and affinity to α₁-, α₂- and β₁-adrenoceptors. The results suggest that the antiarrhythmic and hypotensive effects of these compounds are related to their adrenolytic but not spasmolytic properties.