Ranise A, Bondavalli F, Schenone P, Ciarallo G, Marmo E, Ruta A, D'Angelo G, De Marco G
Farmaco Sci. 1982 Apr;37(4):223-39. doi: 10.1002/chin.198239245.
The synthesis of three series of N-monosubstituted urethanes of 6-cis-dialkylamino-1,3,3-trimethyl-2-oxabicyclo [2.2.2] octan-5-transols (IV), (V) and (VI) (dialkylamino = pyrrolidino, piperidino, morpholino) by reaction of the corresponding aminoalcohols with alkyl or aryl isocyanates, is described. A number of compounds (IV) and (V) showed remarkable hypotensive and bradycardic activity in rats, whereas (IV c) showed infiltration anesthesia and (IV n) antiarrhythmic activity in mice comparable to those of lidocaine. Antiacetylcholine activity in vitro is also reported.
描述了通过相应的氨基醇与烷基或芳基异氰酸酯反应合成三个系列的6-顺式-二烷基氨基-1,3,3-三甲基-2-氧杂双环[2.2.2]辛烷-5-反式醇（IV）、（V）和（VI）（二烷基氨基 = 吡咯烷基、哌啶基、吗啉基）的N-单取代脲烷。许多化合物（IV）和（V）在大鼠中表现出显著的降压和心动过缓活性，而（IV c）在小鼠中表现出浸润麻醉作用，（IV n）表现出与利多卡因相当的抗心律失常活性。还报道了体外抗乙酰胆碱活性。
