Mariani E, Bondavalli F, Schenone P, Benincasa T, Vitagliano S, Marmo E
Istituto di Scienze Farmaceutiche, Università di Genova, Italy.
Farmaco. 1989 May;44(5):503-10.
The synthesis of 1,3,3-trimethyl-N-[(2-pyridyl)methyl]-2- oxabicyclo [2.2.2]octan-6-amine (II) (exo, endo mixture) starting from 1,3,3-trimethyl-N-nitro-2-oxabicyclo [2.2.2]octan-6-imine (I), as well as of a series of amides (III) derived from the above amine, is described. Some compounds (III) showed remarkable depressant and antiarrhythmic activities in rats and mice, respectively, whereas the clofibric acid amide (III e) showed an appreciable hypolipidemic activity in rats. Moreover, the above compounds usually exhibited a moderate infiltration anesthesia in mice, as well as a weak hypotensive and bradycardic activity in rats.
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（I）开始合成1,3,3-三甲基-N-[(2-吡啶基)甲基]-2-氧杂双环[2.2.2]辛烷-6-胺（II）（外消旋体、内消旋体混合物）以及一系列由上述胺衍生的酰胺（III）的过程。一些化合物（III）分别在大鼠和小鼠中表现出显著的镇静和抗心律失常活性，而氯贝酸酰胺（III e）在大鼠中表现出明显的降血脂活性。此外，上述化合物通常在小鼠中表现出中度浸润麻醉作用，在大鼠中表现出较弱的降压和心动过缓活性。
