Gupta Arun, Mishra Pradeep, Kashaw Sushil K, Jatav Varsha, Stables J P
Pharmaceutical Chemistry Division, Department of Pharmaceutical Sciences, Dr. H.S.Gour University, Sagar, MP 470003, India.
Eur J Med Chem. 2008 Apr;43(4):749-54. doi: 10.1016/j.ejmech.2007.05.008. Epub 2007 Jun 3.
A series of 3-aryl amino/amino-4-aryl-5-imino-Delta(2)-1,2,4-thiadiazoline have been synthesized using an appropriate synthetic route and characterized by elemental analyses and spectral data. The anticonvulsant activity of all the synthesized compounds was evaluated against maximal electroshock induced seizures (MES) and subcutaneous pentylenetetrazole (ScPTZ) induced seizure models in mice. The neurotoxicity was assessed using the rotorod method. All the test compounds were administered at doses of 30, 100, and 300 mg/kg body weight and the anticonvulsant activity was noted at 0.5 and 4 h time intervals after the drug administration. Some of the compounds were evaluated for the Phenobarbitone induced hypnosis potentiation test. Among the compounds tested, all except 2h showed protection from MES seizures, whereas only 3b was found to be active in the ScPTZ test.
通过适当的合成路线合成了一系列3-芳基氨基/氨基-4-芳基-5-亚氨基-Δ(2)-1,2,4-噻二唑啉，并通过元素分析和光谱数据对其进行了表征。在小鼠中，针对最大电休克诱导惊厥（MES）和皮下注射戊四氮（ScPTZ）诱导惊厥模型评估了所有合成化合物的抗惊厥活性。使用转棒法评估神经毒性。所有测试化合物均以30、100和300mg/kg体重的剂量给药，并在给药后0.5和4小时的时间间隔记录抗惊厥活性。对部分化合物进行了苯巴比妥诱导催眠增强试验评估。在所测试的化合物中，除2h外均对MES惊厥有保护作用，而在ScPTZ试验中仅发现3b具有活性。
