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Letters in Drug Design & Discovery


ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

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

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

Volume 10 , Issue 8 , 2013

Page: [783 - 791] Pages: 9

DOI: 10.2174/15701808113109990020

Price: $65


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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