2-（取代亚氨基）噻唑烷-4-酮的抗惊厥活性
Anticonvulsant activity of 2-(substituted-imino)thiazolidin-4-ones.
作者信息
Gong G-H, Wang D, Zhang J-F, Wei C-X, Quan Z-S
机构信息
College of Pharmacy, Yanbian University, Yanji, China.
Institute of Medicinal Chemistry and Pharmacology, Inner Mongolia University for Nationalities, Tongliao, China.
出版信息
Drug Res (Stuttg). 2014 Jan;64(1):5-9. doi: 10.1055/s-0033-1349095. Epub 2013 Aug 16.
A novel series of 2-(substituted-imino)thiazolidin-4-ones were synthesized and evaluated for anticonvulsant activity using the maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole (Sc-PTZ) assays and their neurotoxicity was measured by the rotarod test. The results of these tests demonstrated that 2-(4-(pentyloxy)phenylimino)thiazolidin-4-one (5d) was the most potent anticonvulsant, with ED50 value of 18.5 mg/kg and 15.3 mg/kg in the MES and Sc-PTZ tests, and protective index (PI=TD50/ED50) values of 10.6 and 12.8 respectively. 5d was much safer than a reference drug Carbamazepine.
合成了一系列新型的2-(取代亚氨基)噻唑烷-4-酮，并使用最大电休克惊厥（MES）和皮下注射戊四氮（Sc-PTZ）试验评估其抗惊厥活性，通过转棒试验测量其神经毒性。这些试验结果表明，2-(4-(戊氧基)苯基亚氨基)噻唑烷-4-酮（5d）是最有效的抗惊厥剂，在MES和Sc-PTZ试验中的ED50值分别为18.5mg/kg和15.3mg/kg，保护指数（PI=TD50/ED50）值分别为10.6和12.8。5d比参比药物卡马西平安全得多。
Zotero 插件