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.
Letters in Drug Design & Discovery
Title:Antiepileptic Activity of Novel 2-(substituted benzylidene)-7-(4- fluorophenyl)-5-(furan-2-yl)-2H-thiazolo[3,2-a]pyrimidin-3(7H)-one Derivatives
Volume: 10 Issue: 3
Author(s): T. Panneer Selvam, V. Karthick, P. Vijayaraj Kumar and M. Ashraf Ali
Affiliation:
Keywords: Thiazolopyrimidine; Antiepilepsy; Neurotoxicity.
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.
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Panneer Selvam T., Karthick V., Vijayaraj Kumar P. and Ashraf Ali M., Antiepileptic Activity of Novel 2-(substituted benzylidene)-7-(4- fluorophenyl)-5-(furan-2-yl)-2H-thiazolo[3,2-a]pyrimidin-3(7H)-one Derivatives, Letters in Drug Design & Discovery 2013; 10 (3) . https://dx.doi.org/10.2174/1570180811310030003
DOI https://dx.doi.org/10.2174/1570180811310030003 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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