摘要
为了寻找高效的抗神经毒剂梭曼的药物,本文根据HI-6为代表的双吡啶醛肟季铵盐类重活化剂的构效关系及作用机理,设计并合成了22个单吡啶醛肟双季铵盐,这22个目标化合物均系首次报道,合成产物经元素分析及光谱分析证实结构。初步的生物试验表明,某些化合物具有较好的预防和缓解神经毒剂中毒的作用。
In an effort to search for more potent and less toxic antidotes for soman poisoning,twenty two N-[[[2-(hydroxyimino)-methyl]pyridinio]-methoxy]methyl-N, N-dimethyl-3,4-substutited anilinium diivdides were synthesized.All these title compounds were first obtained from biquaternization.Two kinds of mothods were used and evaluated. Quaternizations did not occur when powerful electron-withdrawing groups were present on the aromatic ring or when the ring bore an ortho-substituted group.In comparison with HI-6 and 2-PAM, seven of the compounds were superior to 2-PAM in reactivating human erythrocyte acetylcholinesterase inhibited by soman,but they were less potent than HI-6.
出处
《中国药物化学杂志》
CAS
CSCD
1991年第2期34-37,共4页
Chinese Journal of Medicinal Chemistry
