Synthesis and Evaluation of In Vivo Anticonvulsant Activity of 2,5- Disubstituted-1,3,4-Oxadiazole Derivatives
Kikkeri P. Harish,
Kikkeri N. Mohana,
B. Madhava Reddy,
Nagula Naresh Kumar.
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.
Keywords: Synthesis, 1, 3, 4-oxadiazole, Anticonvulsant activity, Neurotoxicity, Rotorod.
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