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Eur J Med Chem. 2009 Feb;44(2):809-17. doi: 10.1016/j.ejmech.2008.05.019. Epub 2008 Jul 2.

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

Author information

1
Faculty of Chemistry, Rzeszów University of Technology, 6 Powstańców Warszawy Avenue, 35-959 Rzeszów, Poland. ggroszek@prz.edu.pl

Abstract

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 alpha(1)-, alpha(2)- and beta(1)-adrenoceptors' binding affinities. All compounds significantly decrease systolic and diastolic blood pressure, and possess antiarrhythmic activity and affinity to alpha(1)-, alpha(2)- and beta(1)-adrenoceptors. The results suggest that the antiarrhythmic and hypotensive effects of these compounds are related to their adrenolytic but not spasmolytic properties.

PMID:
18599160
DOI:
10.1016/j.ejmech.2008.05.019
[Indexed for MEDLINE]

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