某些1,3-苯并二恶唑衍生物的合成及其肾上腺素β-阻断活性
Synthesis and adrenergic beta-blocking activity of some 1,3-benzodioxole derivatives.
作者信息
Tatsuno H, Goto K, Shigenobu K, Kasuya Y, Obase H
出版信息
J Med Chem. 1977 Mar;20(3):394-7. doi: 10.1021/jm00213a015.
PMID:15112
Abstract
A series of 1,3-benzodioxole derivatives was synthesized. We found four compounds (2,3,10 and 11 in Table IV) to have about the same order of beta-blocking activity as that of sotalol. In addition, it is of interest that some of the compounds (2-4) were found to have hypotensive activites, although they were about one-tenth of that of hydralazine. Sotalol did not produce any change in blood pressure, and propranolol raised the blood pressure.
摘要
合成了一系列1,3 - 苯并二恶唑衍生物。我们发现四种化合物（表IV中的2、3、10和11）具有与索他洛尔大致相同顺序的β - 阻断活性。此外，有趣的是，发现一些化合物（2 - 4）具有降压活性，尽管它们的活性约为肼屈嗪的十分之一。索他洛尔未引起血压任何变化，而普萘洛尔使血压升高。
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