Search for CNS active agents: synthesis of N,N'-bis-[potassium-alkyl/aryl carboxylate]-5-arylidene barbituric acids.

5-Arylidene barbituric acids (1--5, Fig. 1) were obtained by the Perkin's condensation between the corresponding aryl aldehyde and active methylene group of barbituric acid. By the condensation of these 5-arylidene barbituric acids with different alkyl/aryl-chloroacids, fifteen new N,N'bis[potassium-alkyl/aryl carboxylate]-5-arylidene barbituric acids (6--8 Fig. 1) were prepared. Eight of the fifteen final compounds were screened for their pharmacological actions on CNS. They have shown irregular behavioral changes on the CNS; some of them were the CNS stimulants, whereas others were CNS depressants at 1/5 of ALD50 dose level (316--1000 g/kg).