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

作者：Selvam T Panneer^*; Karthick V; Kumar P Vijayaraj; Ali M Ashraf

来源：Letters in Drug Design and Discovery, 2013, 10(3): 204-211.

• Thiazolopyrimidine
• Antiepilepsy
• Neurotoxicity

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, H-1 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.

• 出版日期2013-3