Studies on cerebral protective agents. II. Novel 4-arylpyrimidine derivatives with anti-anoxic and anti-lipid peroxidation activities. (2).
In a search for new cerebral protective agents with anti-anoxic (AA) and anti-lipid peroxidation (ALP) activities, a series of 4-arylpyrimidines, bearing an amino moiety in the C-5 position of the pyrimidine nucleus, was synthesized and tested for AA and ALP activities. Among them, 6-methyl-5-(4-methylpiperazin-1-ylcarbonyl)-4-(3-nitrophenyl )-2-phenylpyrimidin e (41, FK360) was most effective on both assays and on arachidonate-induced cerebral edema in rats. Structure-activity relationships in regard to AA activity of this series of compounds are also discussed.
Kuno
A
A
New Drug Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., Osaka, Japan.
Sugiyama
Y
Y
Katsuta
K
K
Sakai
H
H
Takasugi
H
H
D000818:Animals; D002534:Hypoxia, Brain / Q000188:drug therapy*; D007928:Lethal Dose 50; D015227:Lipid Peroxidation / Q000187:drug effects*; D051379:Mice; D008813:Mice, Inbred ICR; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D051381:Rats; D013329:Structure-Activity Relationship
D011743:Pyrimidines