Synthesis of novel 1-5-(4-methoxy-phenyl)-1,3,4]oxadiazol-2-yl]-piperazine derivatives and evaluation of their in vivo anticonvulsant activity

Harish, K. P. and Mohana, K. N. and Mallesha, L. and Prasanna Kumar, B. N. (2013) Synthesis of novel 1-5-(4-methoxy-phenyl)-1,3,4]oxadiazol-2-yl]-piperazine derivatives and evaluation of their in vivo anticonvulsant activity. European Journal of Medicinal Chemistry, 65. 276 - 283. ISSN 0223-5234

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Abstract

A series of novel 1-5-(4-methoxy-phenyl)-1,3,4]oxadiazol-2-yl]-piperazine derivatives 8(a�o) were synthesized and 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 seizure (MES) model in male wistar rats and compared with the standard drug phenytoin. The neurotoxic effects were determined by rotorod test by using mice. Compounds 8d, 8e, 8f and 8h 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. The pharmacophore model was used to validate the anticonvulsant activity of the synthesized molecules.

Item Type:	Article
Uncontrolled Keywords:	2,5-Disubstituted-1,3,4-oxadiazole, Sulfonyl Chloride, MES, Anticonvulsant
Subjects:	C Chemical Science > Chemistry
Divisions:	Department of > Chemistry
Depositing User:	Arshiya Kousar Library Assistant
Date Deposited:	12 Dec 2019 05:37
Last Modified:	24 Dec 2019 07:04
URI:	http://eprints.uni-mysore.ac.in/id/eprint/10182

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