Faculty of Chemistry, Rzeszów University of Technology, 6 Powstańców Warszawy Avenue, 35-959 Rzeszów, Poland.
Eur J Med Chem. 2009 Dec;44(12):5103-11. doi: 10.1016/j.ejmech.2009.07.012. Epub 2009 Jul 21.
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 alpha(1)-, alpha(2)- and beta(1)-adrenoceptors binding affinities. The antagonist potency of the new compounds was compared with carvedilol and (RS)-9.
(2RS)-1-(5-甲氧基-1H-吲哚-4-基氧基)-3-(2-(2-甲氧基苯氧基)乙基氨基)-2-丙醇和(2RS)-1-(7-甲氧基-1H-吲哚-4-基氧基)-3-(2-(2-甲氧基苯氧基)乙基氨基)-2-丙醇及其对映体,1-(1H-吲哚-4-基氧基)-3-(2-(2-甲氧基苯氧基)乙基氨基)-2-丙醇((RS)-9)的类似物的合成。对化合物进行了电描记法、抗心律失常、降压和松弛活性以及α(1)-、α(2)-和β(1)-肾上腺素受体结合亲和力的测试。新化合物的拮抗剂效力与卡维地洛和(RS)-9进行了比较。