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具有降压、局部麻醉、抗心律失常及其他活性的5-[[ω-(二烷基氨基)烷氧基]亚甲基]-1,3,3-三甲基-2-氧杂双环[2.2.2]辛烷-6-酮

5-[[omega-(Dialkylamino)alkoxy]methylene]-1,3,3-trimethyl-2- oxabicyclo [2.2.2.]octan-6-ones with hypotensive, local anesthetic, antiarrhythmic and other activities.

作者信息

Schenone S, Bruno O, Ranise A, Bondavalli F, D'Amico M, Piu M, Filippelli W, Berrino L

机构信息

Istituto di Scienze Farmaceutiche dell'Università, Genova, Italy.

出版信息

Farmaco. 1994 Sep;49(9):541-4.

PMID:7811348
Abstract

The synthesis of 5-[[omega-(dialkylamino)alkoxy]methylene]-1,3,3-trimethyl-2- oxabicyclo[2.2.2]octan-6-ones by reaction of (+)-5-(hydroxymethylene)-1,3,3-trimethyl-2-oxabicyclo[2.2.2]octan- 6-one with a series of omega-(chloroalkyl)dialkylamines in the presence of potassium carbonate is described. Some compounds showed strong hypotensive, local anesthetic and antiarrhythmic activity in rats and mice, as well as moderate analgesic, antipyretic and in vitro platelet antiaggregating activity.

摘要

描述了通过(+)-5-(羟基亚甲基)-1,3,3-三甲基-2-氧杂双环[2.2.2]辛烷-6-酮与一系列ω-(氯烷基)二烷基胺在碳酸钾存在下反应合成5-[[ω-(二烷基氨基)烷氧基]亚甲基]-1,3,3-三甲基-2-氧杂双环[2.2.2]辛烷-6-酮。一些化合物在大鼠和小鼠中表现出强烈的降压、局部麻醉和抗心律失常活性,以及中等程度的镇痛、解热和体外血小板抗聚集活性。

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