Synthesis and Evaluation of In Vivo Anticonvulsant Activity of 2,5- Disubstituted-1,3,4-Oxadiazole Derivatives

Title:Synthesis and Evaluation of In Vivo Anticonvulsant Activity of 2,5- Disubstituted-1,3,4-Oxadiazole Derivatives

Volume: 10 Issue: 8

Author(s): Kikkeri P. Harish, Kikkeri N. Mohana, Lingappa Mallesha, B. Veeresh, B. Madhava Reddy and Nagula Naresh Kumar

Affiliation:

Keywords: Synthesis, 1, 3, 4-oxadiazole, Anticonvulsant activity, Neurotoxicity, Rotorod.

Abstract: A series of new 2,5-disubstituted-1,3,4-oxadiazole derivatives 8(a-o) was synthesized by the reaction of 1-(5- phenyl-1,3,4-oxadiazol-2-yl)piperazine with various sulfonyl chlorides. The synthesized compounds were characterized by elemental analyses, ¹H NMR, ¹³C NMR and mass spectral studies. The newly synthesized compounds were screened for their anticonvulsant activity against maximal electroshock (MES) seizure method and compared with the standard drug phenytoin. The neurotoxic effects were determined by rotorod test. Compounds 8d, 8e and 8f were found to be most potent of this series. The same compounds showed no neurotoxicity at the maximum dose administered (100 mg/kg). The efforts were also made to establish the structure activity relationships among synthesized compounds.

Cite this article as:

Harish P. Kikkeri, Mohana N. Kikkeri, Mallesha Lingappa, Veeresh B., Reddy Madhava B. and Kumar Naresh Nagula, Synthesis and Evaluation of In Vivo Anticonvulsant Activity of 2,5- Disubstituted-1,3,4-Oxadiazole Derivatives, Letters in Drug Design & Discovery 2013; 10 (8) . https://dx.doi.org/10.2174/15701808113109990020