Studies on Cerebral Protective Agents. VI.Synthesis of Novel 4-(4-Nitrobenzoyl)pyrimidine and Related Compounds with Anti-anoxic Activity

Abstract

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-phenylpyrimidine (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.