具有潜在β-肾上腺素能阻断活性的萘并呋喃衍生物
[Naphthofuran derivatives with potential beta-adrenolytic activity].
作者信息
Garuti L, Ferranti A, Giovanninetti G, Gaggi R
出版信息
Farmaco Sci. 1983 Jul;38(7):527-32.
PMID:6137412
Abstract
1-(Naphtho[1,2-b]furan-2-yl)-2-(isopropylamino)ethanol (II) and 1-(naphtho[2,3-b]furan-2-yl)-2-(isopropylamino)ethanol (III) show low beta-adrenergic blocking activity and unlike the naphtho [2,1-b]furan derivatives (1,2) do not appear to give rise to metabolites with high beta-adrenoceptor inhibitory properties. The inclusion of the --OCH2-- moiety in an aromatic nucleus larger than the benzofuran system (bufuralol, Ro 3-3528) caused loss of the biological activity.
摘要
1-（萘并[1,2-b]呋喃-2-基）-2-（异丙氨基）乙醇（II）和1-（萘并[2,3-b]呋喃-2-基）-2-（异丙氨基）乙醇（III）显示出低β-肾上腺素能阻断活性，并且与萘并[2,1-b]呋喃衍生物（1,2）不同，似乎不会产生具有高β-肾上腺素能受体抑制特性的代谢物。在比苯并呋喃系统更大的芳环中引入--OCH2--部分（布呋洛尔，Ro 3-3528）导致生物活性丧失。
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