[Tert-aminoalkyl derivatives of quinoxalinones, aza- and diazaquinoxalinones with analgesic activity].
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.
Mulé
A
A
Istituto di Tecnica Farmaceutica, Università di Sassari.
Pirisino
G
G
Manca
P
P
Satta
M
M
Peana
A
A
Savelli
F
F
D000700:Analgesics / Q000138:chemical synthesis*; D000818:Animals; D001372:Aza Compounds / Q000138:chemical synthesis / Q000494:pharmacology / Q000633:toxicity; D055598:Chemical Phenomena; D002621:Chemistry; D005260:Female; D007928:Lethal Dose 50; D051379:Mice; D010147:Pain Measurement; D011810:Quinoxalines / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity
D000700:Analgesics; D001372:Aza Compounds; D011810:Quinoxalines
Terz-amminoalchilderivati di chinossalinoni, aza e diazachinossalinoni ad attività analgesica.