Water soluble 2,4,6-trinitrophenylbarbiturates of moderate therapeutic index as anticonvulsant / hypnotic agents*

摘要

Water soluble 2,4,6-trinitrophenylbarbiturates have been synthesised through one pot synthesis in good yield of high purity from the ethanolic solution of l-chloro-2,4,6-trinitrobenzene, barbituric acid and amines (triethylamine, tri-n-butylamine & triethanolamine). The structures of the synthesised barbiturates have been identified from uv-vis, ir, pmr, 13C nmr, mass and single crystal X-ray data. Elemental analysis and other qualitative tests have also been carried out to confirm the structures. The anticonvulsant activity of the synthesised barbiturates has been tested by Maximal Electro Shock method. Reduction in extensor phase of convulsion has been noticed for the synthesised barbiturates. An initial assessment of toxic manifestation has been made through the determination of LD_50 values in animal model. The drugs fall under class 4 (LD_50 > 1500 mg / kg). The animals did not show any sign of acute toxicity and behavioral changes. Therapeutic dose of the drugs induces hypnosis in albino mice.