作者:Arun Gupta、Pradeep Mishra、S.N. Pandeya、Sushil K. Kashaw、Varsha Kashaw、James P. Stables
DOI:10.1016/j.ejmech.2008.06.015
日期:2009.3
A series of new substituted 1,2,4-thiadiazoles were synthesized by appropriate route and screened for anticonvulsant, neurotoxic and sedative-hypnotic activity. The structures of the synthesized compounds were confirmed by IR spectroscopy, 13C NMR and elemental (nitrogen and sulphur) analysis. After i.p. injection of the compounds to mice or rate at doses of 30, 100, and 300 mg/kg, body weights were
通过适当的途径合成了一系列新的取代的1,2,4-噻二唑,并筛选了其抗惊厥,神经毒性和镇静催眠活性。合成的化合物的结构通过IR光谱,13 C NMR和元素(氮和硫)分析确认。将化合物经腹腔注射给小鼠或以30、100和300 mg / kg的剂量给药后,在0.5和0.5倍后分别在最大电击诱发的癫痫发作(MES)和皮下戊四唑(scPTZ)诱发的癫痫发作模型中检查体重。 4小时 采用Rotorod法和苯巴比妥诱导的催眠作用增强研究来分别研究神经毒性和镇静催眠活性。0.5h后除4g外的所有化合物均显示出对MES筛选的保护。化合物3a – c,4a – c在100 mg / kg剂量ip时有活性,而其余化合物在300 mg / kg时显示活性。0.5 g后,除3 g外,所有14种化合物均显示出100和300 mg / kg的神经毒性。化合物3b和4b在4小时后显示NT。两种化合物3b和4g的 睡眠时间显着增加(p