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

The synthesis of (2 RS)-1-(1 H-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 α 1-, α 2- and β 1-adrenoceptors' binding af...

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Veröffentlicht in:European journal of medicinal chemistry 2009-02, Vol.44 (2), p.809-817
Hauptverfasser: Groszek, Grażyna, Bednarski, Marek, Dybała, Małgorzata, Filipek, Barbara
Format: Artikel
Sprache:eng
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Zusammenfassung:The synthesis of (2 RS)-1-(1 H-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 α 1-, α 2- and β 1-adrenoceptors' binding affinities. All compounds significantly decrease systolic and diastolic blood pressure, and possess antiarrhythmic activity and affinity to α 1-, α 2- and β 1-adrenoceptors. The results suggest that the antiarrhythmic and hypotensive effects of these compounds are related to their adrenolytic but not spasmolytic properties. [Display omitted] The synthesis of ( RS)- 9 and its enantiomers has been described and tested for electrocardiographic, antiarrhythmic, hypotensive and spasmolytic activities as well as for α 1-, α 2- and β 1-adrenoceptors' binding affinities.
ISSN:0223-5234
1768-3254
DOI:10.1016/j.ejmech.2008.05.019