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Synthesis of new 2,5-disubstituted-1,3,4-thiadiazole derivatives and their in vivo anticonvulsant activity

Abstract

A series of 2,5-disubstituted-1,3,4-thiadiazole derivatives were synthesized by the reaction of 3-(2-cyanopropan-2-yl)-N-(5-(piperazine-1-yl)-1,3,4-thiadiazol-2-yl)benzamide with various sulfonyl chlorides and evaluated for their anticonvulsant activity in MES test. Rotorod method was employed to determine the neurotoxicity. The purity of the compounds is confirmed on the basis of their elemental analysis. The structures of all the new compounds are established on the basis of 1H NMR and mass spectral data. Out of fifteen compounds, three were found to be potent anticolvunstants. The same compounds showed no neurotoxicity at the maximum dose administered (100 mg/kg).

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Correspondence to K. P. Harish.

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Harish, K.P., Mohana, K.N. & Mallesha, L. Synthesis of new 2,5-disubstituted-1,3,4-thiadiazole derivatives and their in vivo anticonvulsant activity. Russ J Bioorg Chem 40, 97–105 (2014). https://doi.org/10.1134/S1068162014010051

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  • DOI: https://doi.org/10.1134/S1068162014010051

Keywords

  • 1,3,4-thiadiazole
  • anticonvulsant
  • neurotoxicity