Studies on cerebral protective agents. VI. Synthesis of novel 4-(4-nitrobenzoyl)pyrimidine and related compounds with anti-anoxic activity.
Novel pyrimidine derivatives, possessing linkages between the aryl group and the pyrimidine nucleus at the C-4 position, were prepared and tested for anti-anoxic (AA) activity in mice. Among them, 5-(4-methylpiperazin-1-ylcarbonyl)-4-(4-nitrobenzoyl)-2-p henylpyrimidine (2f, FR76659) possessed significant AA activity (10-100 mg/kg, i.p.) with low acute toxicity (LD50 > 1000 mg/kg, i.p.). Structure-activity relationships in regard to AA activity of this series of compounds were examined.
Ohkubo
M
M
New Drug Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., Osaka, Japan.
Kuno
A
A
Sakai
H
H
Sugiyama
Y
Y
Takasugi
H
H
D000818:Animals; D002534:Hypoxia, Brain / Q000188:drug therapy*; D007928:Lethal Dose 50; D051379:Mice; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity
D011743:Pyrimidines