Abstract |
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.
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Authors | A Kuno, Y Sugiyama, K Katsuta, H Sakai, H Takasugi |
Journal | Chemical & pharmaceutical bulletin
(Chem Pharm Bull (Tokyo))
Vol. 40
Issue 9
Pg. 2423-31
(Sep 1992)
ISSN: 0009-2363 [Print] Japan |
PMID | 1446365
(Publication Type: Journal Article)
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Chemical References |
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Topics |
- Animals
- Hypoxia, Brain
(drug therapy)
- Lethal Dose 50
- Lipid Peroxidation
(drug effects)
- Mice
- Mice, Inbred ICR
- Pyrimidines
(chemical synthesis, pharmacology, toxicity)
- Rats
- Structure-Activity Relationship
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