Synthesis of some derived thiazolidin-4-one, azetidin-2-one and 1,3,4-oxadiazole ring systems from Isoninicotinic acid hydrazide: A novel class of potential anticonvulsant agents

BySadaf Jamal Gilani, Ozair Alam, Suroor Ahmad Khan, Nadeem Siddiqui, Harish Kumar

Abstract

A series of Isoninicotinic acid hydrazide (INH) incorporated derivatives of thiazolidin-4-one (2a-h,3a-h), azetidin-2-one (4a-h) and 1,3,4-oxadiazole (5a-h) has been synthesized using an appropriate synthetic route and characterized by elemental analysis 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 rota-rod 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 4h time intervals after the drug administration. All the compounds were active in MES and a majority of compounds were active in scPTZ test. All compounds were less neurotoxic than the standard drug phenytoin.

 

Key Words : Thiazolidin-4-one, azetidin-2-one, 1,3,4-oxadiazole, maximal electroshock (MES), subcutaneous pentylenetetrazole (scPTZ).

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