Synthesis and evaluation of in vivo anticonvulsant activity of 2,5-disubstituted-1,3,4-oxadiazole derivatives

Harish, K. P. and Mohana, K. N. and Mallesha, L. and Veeresh, B. and Madhava Reddy, B. and Naresh Kumar, N. (2013) Synthesis and evaluation of in vivo anticonvulsant activity of 2,5-disubstituted-1,3,4-oxadiazole derivatives. Letters in Drug Design and Discovery, 10 (8). pp. 783-791.

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Official URL: http://doi.org/10.2174/15701808113109990020

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.

Item Type: Article
Uncontrolled Keywords: article, male, priority journal, animal experiment, animal model, controlled study, drug screening, nonhuman, rat, 1, unclassified drug, drug synthesis, structure activity relation, 3, mass spectrometry, 4 oxadiazole derivative, anticonvulsant activity, drug potency, neurotoxicity, seizure, in vivo study, piperazine derivative, proton nuclear magnetic resonance, carbon nuclear magnetic resonance, phenytoin, benzene derivative, electric shock, rotarod test, 1 (2, 1 (4 phenoxybenzene)sulfonyl] 4 (5 phenyl 1, 1 2 nitro 4 (trifluoromethyl)phenyl]sulfonyl] 4 (5 phenyl 1, 4 oxadiazol 2 yl)piperazine, 5 dichlorothiophen 3 yl)sulfonyl] 4 (5 phenyl 1, sulfone derivative
Subjects: C Chemical Science > Chemistry
Divisions: Department of > Chemistry
Depositing User: Arshiya Kousar Library Assistant
Date Deposited: 20 Sep 2019 10:14
Last Modified: 20 Sep 2019 10:14
URI: http://eprints.uni-mysore.ac.in/id/eprint/7966

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