Synthesis of indazole substituted-1,3,4-thiadiazoles and their anticonvulsant activity

Objectives

To synthesize a new series of indazole substituted-1,3,4-thiadiazole derivatives 7(a-l) and test the anticonvulsant activity against maximal electroshock (MES) seizure model in male Wistar rats.

Methods

New compounds were synthesized by the reaction of indazole substituted-1,3,4-thiadiazoles with various sulfonyl chlorides. The purity of the compounds was confirmed on the basis of their elemental analysis. Chemical structures of all the new compounds were established by ¹H NMR and mass spectral data. Anticonvulsant study was done by MES seizure model and rotorod method was employed to determine the neurotoxicity.

Results

All the compounds were synthesized in good yield. Out of twelve compounds, 7b and 7d are found to be most potent of this series. The same compounds showed no neurotoxicity at the maximum dose administered (100 mg/kg).

Conclusions

The results obtained justify the usage of these compounds from their promising anticonvulsant activity. Further studies are needed to fully characterize the toxicity and the mechanisms involved with the anticonvulsant activity and neurotoxicity of these compounds.