Novel 4-phenoxy-2-(1-piperazinyl)quinazolines as potent anticonvulsive and antihypoxic agents.
A series of 4-phenoxy-2-(1-piperazinyl)quinazolines was synthesized and examined for anticonvulsive and antihypoxic activities. Many of the compounds exhibited potent anticonvulsive activity comparable to that of carbamazepine or phenytoin. Among them, 4-phenoxy-2-(4-propyl-1-piperazinyl)quinazoline (5w) was selected as the most promising candidate antiepileptic drug with few side effects. It seemed that potent anticonvulsive activity was a prerequisite for potent antihypoxic activity.
Hori
M
M
Pharmaceuticals Research Center, Kanebo Ltd., Osaka, Japan.
Iemura
R
R
Hara
H
H
Ozaki
A
A
Sukamoto
T
T
Ohtaka
H
H
D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis*; D055598:Chemical Phenomena; D002621:Chemistry; D004597:Electroshock; D000860:Hypoxia / Q000188:drug therapy*; 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; D013329:Structure-Activity Relationship
D000927:Anticonvulsants; D010879:Piperazines; D011799:Quinazolines