SYNTHESIS, CHARACTERIZATION AND EVALUATION OF ANTICONVULSANT / HYPNOTIC ACTIVITY AND TOXICITY EFFECT: TRIBUTYLAMMONIUM 2,6- DIOXO-5-(2,4,6–TRINITROPHENYL)–1,2,3,6 TETRAHYDROPYRIMIDIN-4-OLATE

Abstract

A new type of barbiturate (a pyrimidine derivative) has been prepared through one potsynthesis from the ethanolic solution of 1-chloro-2,4,6-trinitroben-zene, barbituric acid and Tributylamine. The mechanism of the formation of the reported barbiturate involves an intermediate sigma complex formation and proton abstraction reactions. The structure of the titlebarbiturate has been identified from UV–Vis, FT-IR, 1 H NMR, 13 C NMR and elemental analysisdata. The anticonvulsant activity of the synthesized barbiturate has been tested by MaximalElectro Shock method on albino rats. Reduction in extensor phase of convulsion has beennoticed for the synthesised barbiturates. An initial assessment of toxic manifestation has beenmade through the determination of LD 50 values in animal model. The drugs fall under class (LD 50 >1500 mg kg -1 ). The animals did not show any sign of acute toxicity and behavioural changes. Therapeutic dose of the drugs induces hypnosis in albino mice (dose,100 mg kg -1 ) for a duration of 47 min.