Synthesis and characterization of some heterocyclic schiff bases: potential anticonvulsant agents
作者:Shailendra Pandey、R. S. Srivastava
DOI:10.1007/s00044-010-9441-z
日期:2011.9
over clinically used drugs in sc.PTZ screen (ED50) 6.44, 11.70, 6.47, and 14.16 with (PI > 10). Compound (4b) showed good anticonvulsant activity (ED50) 20.79, but with relatively higher neurotoxicity (PI, 0.57). Compound (1e) was active in both sc.PTZ and in sc.STR seizures. Some selected compounds were subjected to oral MES screen (30 mg kg−1) in rats, most of the compounds showed peak activity after
通过与取代的芳基醛/酮和/环酮的缩合反应合成了一系列3-氨基甲基吡啶的新型席夫碱。筛选这些席夫碱的抗惊厥活性。通过FT-IR,1 H-NMR,光谱学和元素分析证实了合成化合物的化学结构。在采用的各种模型中,观察到许多化合物在以30和100 mg kg -1的剂量腹膜内给药后表现出癫痫发作保护作用。在MES筛选中,我们发现了五种有效的化合物,即(1 c)N-(2-氯苄叉基)(吡啶-3-基)甲胺,(1 f)2-甲氧基-4-(吡啶-3-基甲基亚氨基)甲基}苯酚,(2 a)ñ - (3phenylallylidene)(吡啶-3-基)甲胺,(3 b)3- 1-(吡啶-3- ylmethylimino)乙基}苯胺,和(4一)ñ - (二苯基-亚甲基)(吡啶-3- -yl)甲胺,以(ED 50)11.70、6.39、11.70、8.64和9.13 mg kg -1系列中最活泼的化合物出现,具有高保护指数(PI)>10。四种化合物(1