具有降压及其他活性的1,3,3-三甲基-N-(2-吡啶基)-2-氧杂双环[2.2.2]辛烷-6-胺衍生物
1,3,3-Trimethyl-N-(2-pyridyl)-2-oxabicyclo[2.2.2]octan-6-amine derivatives with hypotensive and other activities.
作者信息
Mariani E, Bruno O, Schenone P, De Santis D, Di Mauro G, Marmo E
出版信息
Farmaco Sci. 1986 Jun;41(6):454-63.
PMID:3743741
Abstract
The synthesis of 1,3,3-trimethyl-N-(2-pyridyl)-2-oxabicyclo-[2.2.2]octan-6-amine (cis, trans mixture) starting from 1,3,3-trimethyl-N-nitro-2-oxabicyclo[2.2.2]octan-6-imine, as well as of a series of amides (V) derived from the above amine, is described. Some compounds (V) showed strong hypotensive activity in rats. Effects on heart rate and antiarrhythmic activity in rats, as well as local anesthetic activity in mice, are also reported.
摘要
描述了从1,3,3-三甲基-N-硝基-2-氧杂双环[2.2.2]辛烷-6-亚胺开始合成1,3,3-三甲基-N-(2-吡啶基)-2-氧杂双环[2.2.2]辛烷-6-胺（顺式、反式混合物）以及一系列由上述胺衍生的酰胺(V)的方法。一些化合物(V)在大鼠中表现出强烈的降压活性。还报道了其对大鼠心率和抗心律失常活性的影响，以及对小鼠的局部麻醉活性。
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