Synthesis and anticonvulsant activity of some novel 3-aryl amino/amino-4-aryl-5-imino-Δ2-1,2,4-thiadiazoline

A series of 3-aryl amino/amino-4-aryl-5-imino-Δ2-1,2,4-thiadiazoline have been synthesized using an appropriate synthetic route and characterized by elemental analyses and spectral data. The anticonvulsant activity of all the synthesized compounds was evaluated against maximal electroshock induced seizures (MES) and subcutaneous pentylenetetrazole (ScPTZ) induced seizure models in mice. The neurotoxicity was assessed using the rotorod method. All the test compounds were administered at doses of 30, 100, and 300 mg/kg body weight and the anticonvulsant activity was noted at 0.5 and 4 h time intervals after the drug administration. Some of the compounds were evaluated for the Phenobarbitone induced hypnosis potentiation test. Among the compounds tested, all except 2h showed protection from MES seizures, whereas only 3b was found to be active in the ScPTZ test.

Graphical abstractA series of 3-aryl amino/amino-4-aryl-5-imino-Δ2-1,2,4-thiadiazoline have been synthesized and evaluated for anticonvulsant activity and neurotoxicity by maximal electroshock induced seizures (MES) and subcutaneous pentylenetetrazole (ScPTZ) induced seizure models in mice. Almost all compounds showed protection against MES induced seizures whereas only 3b was found to be active in ScPTZ test.Figure optionsDownload full-size imageDownload as PowerPoint slide