Mulé A, Pirisino G, Manca P, Satta M, Peana A, Savelli F
Istituto di Tecnica Farmaceutica, Università di Sassari.
Farmaco Sci. 1988 Jul-Aug;43(7-8):613-8.
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.
制备了一系列喹喔啉-2-酮、氮杂喹喔啉-2-酮和二氮杂喹喔啉-2-酮的叔氨基烷基衍生物，这些衍生物在3位带有苄基，以便与类似的3-甲基衍生物在镇痛活性方面进行比较。这种取代产生了各种影响。在化合物（I）和（VI-IX）中发现镇痛活性有预期的增加，但同时毒性也增加。化合物（IV）和（V）因其LD50与ED50有很大差异而备受关注。
