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

被引：19
|
作者：
Groszek, Grazyna [1 ]
Bednarski, Marek [2 ]
Dybala, Malgorzata [3 ]
Filipek, Barbara [2 ]
机构：
[1] Rzeszow Univ Technol, Fac Chem, PL-35959 Rzeszow, Poland
[2] Jagiellonian Univ, Coll Med, Lab Pharmacol Screening, PL-30689 Krakow, Poland
[3] Jagiellonian Univ, Coll Med, Dept Pharmacobiol, PL-30689 Krakow, Poland
来源：
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2009年 / 44卷 / 02期
关键词：
alpha(1)-; alpha(2)-; beta(1)-Adrenoceptor antagonist; Antiarrhythmic; hypotensive and spasmolytic activities; Synthesis; CARVEDILOL BLOCKS; CURRENTS;
D O I：
10.1016/j.ejmech.2008.05.019
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
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. (c) 2008 Elsevier Masson SAS. All rights reserved.
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页码：809 / 817
页数：9
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