Synthesis of 6-(3-substituted-4H-1,2,4-triazol-4-yl)-2-phenylbenzo[d]oxazoles as potential anticonvulsant agents

摘要

A series of 6-(3-substituted-4H-1,2,4-triazol-4-yl)-2-phenylbenzo[d]oxazoles was synthesized. The anticonvulsant effect and neurotoxicity of the compounds were calculated with maximal electroshock (MES) test, subcutaneous pentylenetetrazole (Sc-PTZ), and rotarod tests in intraperitoneally injected mice. Among the synthesized compounds, compound 2-phenyl-6-(4H-1,2,4-triazol-4-yl)benzo[d]oxazole (3a) could be considered the potentially most useful and safe therapeutic compound, with ED₅₀ = 29.6 mg/kg, TD₅₀ = 285 mg/kg, and PI = 9.7. Its neurotoxicity was the lowest of all the synthesized compounds and was also markedly lower than that of the reference drug carbamazepine with PI value of 6.4.