Novel 4-substituted 2-piperazinylquinazolines as potent anticonvulsive and antihypoxic agents.
Several types of quinazoline derivatives were prepared and examined for anticonvulsive and antihypoxic activities. Many compounds showed potent anticonvulsive activity, and their anticonvulsive profile is similar to that of phenytoin. The analysis of quantitative structure-activity relationships indicated that the anticonvulsive activity was parabolically related to the lipophilicity of the compounds. Most of the 4-alkoxyquinazolines showed potent anticonvulsive and antihypoxic activities. It is confirmed that there is a good correlation between the potencies of these activities.
Pharmaceuticals Research Center, Kanebo Ltd., Osaka, Japan.
M
M
Hori
R
R
Iemura
H
H
Hara
A
A
Ozaki
T
T
Sukamoto
H
H
Ohtaka
D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis*; D055598:Chemical Phenomena; D002621:Chemistry; D000860:Hypoxia / Q000188:drug therapy*; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D008815:Mice, Inbred Strains; D010879:Piperazines / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D011799:Quinazolines / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity
D000927:Anticonvulsants; D010879:Piperazines; D011799:Quinazolines