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Letters in Drug Design & Discovery

Editor-in-Chief

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

Antiepileptic Activity of Novel 2-(substituted benzylidene)-7-(4- fluorophenyl)-5-(furan-2-yl)-2H-thiazolo[3,2-a]pyrimidin-3(7H)-one Derivatives

Author(s): T. Panneer Selvam, V. Karthick, P. Vijayaraj Kumar and M. Ashraf Ali

Volume 10 , Issue 3 , 2013

Page: [204 - 211] Pages: 8

DOI: 10.2174/1570180811310030003

Price: $65

Abstract

A series of 2-(substituted benzylidene)-7-(4-fluorophenyl)-5-(furan-2-yl)-2H-thiazolo[3,2-a]pyrimidin-3(7H)- one derivatives were newly synthesized by the reaction of 7-(4-fluoro phenyl)-5-(furan-2-yl)-2H-thiazolo[3,2- a]pyrimidin-3(7H)-one (3) with appropriate substituted benzaldehyde in the presence of anhydrous sodium acetate and glacial acetic acid. Their structures were confirmed by IR, 1H NMR, mass and elemental analyses. These novel thiazolopyrimidine derivatives were screened for their antiepileptic activity by using MES: Maximal Electroshock Seizure test and ScPTZ: Subcutaneous pentylenetetrazole seizures tests. The neurotoxicity was determined by rotorod test. Among these compounds 4f revealed protection in MES at a dose of 30 mg kg-1 and 100 mg kg-1 0.5 h and 4 h after i.p. administration respectively. This molecule provided also protection in the scPTZ at a dose of 300 mg kg-1 in both time intervals.

Keywords: Thiazolopyrimidine; Antiepilepsy; Neurotoxicity.


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