对氰基苯代二氢哒嗪酮的设计，合成及抗惊活性的研究  

STUDY ON THE DESIGN,SYNTHESIS AND ANTICONVULSANT ACTIVITY OF P-CYANOPHENYL-DIHYDROPYRIDAZINONE

作　　者：徐萍[1] 李仁利[1] 冯军[1] 周家驹[1] 

机构地区：[1]北京医科大学药物化学教研室,中国科学院计算机化学开放实验室

出　　处：《中国药物化学杂志》1994年第2期93-96,共4页Chinese Journal of Medicinal Chemistry

摘　　要：在ＣｏＭＦＡ３Ｄ－ＱＳＡＲ研究的基础上设计并合成了对氰基苯代二氢哒嗪酮。对溴苯甲醛与吗啉、氰化钾反应得α－ｐ－溴苯基－４－吗啉基乙腈，再与丙烯腈反应得３－（ｐ－溴代苯基）丙酸。对溴基被氰基取代后与肼反应得目标化合物。其抗惊活性属中等强度，与ＣｏＭＦＡ方法预计值相差较大。On the basis of CoMFA 3D-QSAR studies 6-(p-cyanophenyl)-4,5-dihydro-3(2H)pyridazinone was designed and synthesized.α-(p-bromophenyl)-α-4-morpholineacetonitrile obtained from p-bromobenzaldehyde,morpholine and potassium cyanide,was used to synthesize 3-(p-bromophenyl)-propionic acid by 1,4-addition to acrylonitrile. The bromo group of 3-(pbromophenyl)-propionic aicd was substituted by cyano group to give 3-(p-cyanophenyl)-propionic acid which was then converted into the target compound by reacting with hydrazine.The target compound possessed modest anticonvulsant activity and it was much less potent than the predicted value by the CoMFA method.

关 键 词：对氰基 苯代二氢哒嗪酮 抗惊厥药 合成 

分 类 号：TQ463.24[化学工程—制药化工] R971.6[医药卫生—药品]