[Tert-aminoalkyl derivatives of quinoxalinones, aza- and diazaquinoxalinones with analgesic activity].

Il Farmaco; edizione scientifica Pub Date : 1988-07-01
A Mulé, G Pirisino, P Manca, M Satta, A Peana, F Savelli
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Abstract

A series of tert-aminoalkyl-derivatives of quinoxalin-2-one, aza- and diazaquinoxalin-2-one bearing in position 3 a benzyl group was prepared in order to compare with analogous 3-methyl derivatives as regards analgesic activity. The substitution causes various effects. In compounds (I) and (VI-IX) is found the expected increase in analgesic activity but with contemporaneous rise in toxicity. The compounds (IV) and (V) are of interest due to the presence of a strong separation of DL50 from DE50.

[具有镇痛活性的喹诺沙林酮、杂喹诺沙林酮和重氮喹诺沙林酮的叔胺烷基衍生物]。
制备了一系列喹啉-2- 1、氮杂喹啉-2- 1和二氮喹啉-2- 1的叔胺烷基衍生物,并与类似的3-甲基衍生物进行了镇痛活性比较。这种替代会产生各种各样的影响。在化合物(I)和(VI-IX)中发现预期的镇痛活性增加,但同时毒性增加。化合物(IV)和(V)是由于DL50和DE50之间存在很强的分离而引起的。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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