Synthesis and adrenolytic activity of 1-(1H-indol-4-yloxy)-3-(2-(2-methoxy phenoxy)ethylamino)propan-2-ol analogs and its enantiomers. Part 2

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• 作者：Graż ; yna Groszek ; Agnieszka Nowak-Kró ; l ; Tomasz Wdowik ; Dariusz Ś ; wierczyń ; ski ; Marek Bednarski ; Monika Otto ; Maria Walczak ; Barbara Filipek
• 关键词：Synthesis ; Enantiomers ; α ; ₁- ; α ; ₂- and β ; ₁-Adrenoceptor antagonists ; Cardiovascular and spasmolytic activities
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2009
• 出版时间：December 2009
• 年：2009
• 卷：44
• 期：12
• 页码：5103-5111
• 全文大小：347 K

文摘

The synthesis of (2RS)-1-(5-methoxy-1H-indol-4-yloxy)-3-(2-(2-methoxyphenoxy)ethylamino)propan-2-ol and (2RS)-1-(7-methoxy-1H-indol-4-yloxy)-3-(2-(2-methoxyphenoxy)ethylamino)propan-2-ol and its enantiomers, analogs of 1-(1H-indol-4-yloxy)-3-(2-(2-methoxyphenoxy)ethylamino)propan-2-ol ((RS)-9) is described. Compounds were tested for electrographic, antiarrhythmic, hypotensive and spasmolytic activities as well as for α₁-, α₂- and β₁-adrenoceptors binding affinities. The antagonist potency of the new compounds was compared with carvedilol and (RS)-9.