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.
引用
收藏
页码：809 / 817
页数：9
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