首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis and adrenolytic activity of 1-(1H-indol-4-yloxy)-3-(2-(2-methoxy phenoxy)ethylamino)propan-2-ol analogs and its enantiomers. Part 2.
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Synthesis and adrenolytic activity of 1-(1H-indol-4-yloxy)-3-(2-(2-methoxy phenoxy)ethylamino)propan-2-ol analogs and its enantiomers. Part 2.

机译:1-(1H-吲哚-4-基氧基)-3-(2-(2-甲氧基苯氧基)乙氨基)丙烷-2-醇类似物及其对映异构体的合成和肾上腺素酶活性。第2部分。

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摘要

The synthesis of (2RS)-1-(5-methoxy-1H-indol-4-yloxy)-3-(2-(2-methoxyphenoxy)ethylamino)propan-2-o l and (2RS)-1-(7-methoxy-1H-indol-4-yloxy)-3-(2-(2-methoxyphenoxy)ethylamino)propan-2-o l 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.
机译:(2RS)-1-(5-甲氧基-1H-吲哚-4-基氧基)-3-(2-(2-甲氧基苯氧基)乙氨基)丙烷-2-醇和(2RS)-1-(7-甲氧基-1H-吲哚-4-基氧基)-3-(2-(2-甲氧基苯氧基)乙氨基)丙-2-醇及其对映体,1-(1H-吲哚-4-基氧基)-3-(2描述了-(2-甲氧基苯氧基)乙氨基)丙-2-醇((RS)-9)。测试了化合物的电图,抗心律不齐,降压和痉挛活性,以及​​α(1)-,α(2)-和β(1)-肾上腺素受体的结合亲和力。将新化合物的拮抗剂效力与卡维地洛和(RS)-9进行了比较。

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