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1,3,3-三甲基-5-内-(1-哌啶基或4-吗啉基)-2-氧杂双环[2.2.2]辛烷-6-酮的N-取代O-(3-氨基-2-羟丙基)肟,具有血小板抗聚集和局部麻醉活性。

N-substituted O-(3-amino-2-hydroxypropyl)oximes of 1,3,3-trimethyl-5-endo-(1-piperidinyl or 4-morpholinyl)-2-oxabicyclo [2.2.2]-octan-6-ones with platelet antiaggregating and local anesthetic activities.

作者信息

Schenone S, Bruno O, Ranise A, Bondavalli F, D'Amico M, Parrillo C, Lampa E, Rossi F

机构信息

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

出版信息

Farmaco. 1992 Oct;47(10):1249-62.

PMID:1482516
Abstract

The synthesis of a series of N-substituted O-(3-amino-2-hydroxypropyl)oximes of 1,3,3-trimethyl-5-endo-(1-piperidinyl or 4-morpholinyl)-2-oxabicyclo [2.2.2]octan-6-ones is described. Some of these ethers showed strong local anesthetic activity in mice and platelet antiaggregating activity in vitro comparable to that of acetylsalicylic acid, as well as moderate hypotensive, antiarrhythmic and analgesic activities in rats and mice.

摘要

描述了一系列1,3,3-三甲基-5-内-(1-哌啶基或4-吗啉基)-2-氧杂双环[2.2.2]辛烷-6-酮的N-取代O-(3-氨基-2-羟丙基)肟的合成。其中一些醚类化合物在小鼠中表现出强烈的局部麻醉活性,在体外具有与乙酰水杨酸相当的血小板抗聚集活性,以及在大鼠和小鼠中具有适度的降压、抗心律失常和镇痛活性。

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