1,2-二氢-2-氧代喹啉衍生物的合成及其生理活性的研究  

Synthesis and Physiological Activity of 1,2-Dihydro-2-oxo-quinoline Derivatives

作　　者：叶蕴华[1] 纪建国 邱晓生 刘世熠[3] 张文远[3] 王泽盛 戴秀菊[3] 

机构地区：[1]北京大学化学系 [2]烟台大学生物化学系 [3]中国科学院上海生理所

出　　处：《北京大学学报（自然科学版）》1990年第2期207-213,共7页Acta Scientiarum Naturalium Universitatis Pekinensis

摘　　要：本文用三种不同的方法分别合成了五个尚未见文献报道的1,2-二氢-2-氧代喹啉-4-羧酸酯,同时改进文献方法合成了DL-α-氨基-β-[4-(1,2-二氢-2-氧代喹啉)]丙酸及其中间体。用106只小鼠测定了以上化合物的生理活性,腹腔注射(25～50mg/kg)均未见小鼠行为异常,全部动物均未见注射后24h内死亡现象,其中若干衍生物(25mg/kg,i.p.)可使小鼠呈现适度的降低肛温和呼吸频率生理效应,化合物Ⅴ与Ⅵ作用最显著。Ⅵ与戊巴比妥呈现协同作用表明该类化合物有可能具有外源性促眠效应。Five new esters of 1,2-dihydro-2-oxo-4-quinoline carboxylic acid have been synthesized by using three different methods respectively. An improved method of synthesis was adopted for DL-α-amino-β-[4-(1,2-dihydro-2-oxo-quinoline)] propionic acid, as well as its intermediate compound. The evaluation of all the derivatives was done in 106 mice. Results show that after administration of ⅠⅥ (25-50mg/kg, i. p. ) no abnormal behaviour or mortality could be observed, whereas some of them (25mg/kg, i. p. ) could induce reasonable decreasing of rectal temperature (Ⅰ,Ⅳ, Ⅴ, Ⅵa,Ⅵ) and .respiratory rates (Ⅰ, Ⅲ, Ⅳ, Ⅴ, Ⅵa, Ⅵ) respectively in mice test. The effects of Ⅴ, Ⅵa and Ⅵ seem most prominent. Besides, effects of Ⅵ(25mg/kg, i. p. )could be enhanced by pentobarbital (20mg/kg, i. p. ), but not scopolamine(0.2mg/kg, i. p. ).

关 键 词：喹啉 衍生物 合成 生理活性 促眠 

分 类 号：R971.3[医药卫生—药品]