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Studies on cerebral protective agents. I. Novel 4-arylpyrimidine derivatives with anti-anoxic and anti-lipid peroxidation activities.

作者信息

Kuno A, Sugiyama Y, Katsuta K, Kamitani T, Takasugi H

机构信息

New Drug Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., Osaka, Japan.

出版信息

Chem Pharm Bull (Tokyo). 1992 Jun;40(6):1452-61. doi: 10.1248/cpb.40.1452.

DOI:10.1248/cpb.40.1452
PMID:1394663
Abstract

Novel 4-arylpyrimidine derivatives were synthesized by the oxidation of 4-aryl-1,4-dihydropyrimidines, and their effects on anti-anoxic (AA) activity in mice and anti-lipid peroxidation (ALP) activity in rat brain mitochondria were investigated. Among these compounds, ethyl 6-methyl-2-phenyl-4-(4-pyridyl)-5-pyrimidinecarboxylate (4b) has AA activity (10 mg/kg, i.p.) and ethyl 6-methyl-4-(3-nitrophenyl)-2-phenyl-5-pyrimidinecarboxylate (4f) has ALP activity (73% inhibition at 10(-5) g/ml). The latter compound (100 mg/kg, i.p.) was also effective on arachidonate-induced cerebral edema in rats with comparable potency to that of vitamin E.

摘要

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