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本文设计,合成了2-(E)-取代苯亚甲基环戊酮(Ⅰ)类化合物18个及其Mannich碱盐酸盐(Ⅱ)类化合物11个,其中22个为新化合物。初步药理结果显示:对于角叉菜胶诱发的大鼠足趾水肿,Ⅰ_4,Ⅰ_(12)及Ⅰ_(13)口服有较显著的抑制作用,水溶性Ⅱ类化合物皮下注射有极强的抑制作用,其中Ⅱ_3于50,25和12.5 mg/kg剂量下抑制率分别为95.8%,70.3%和44.2%,它与布洛芬效力(25 mg/bg抑制率72.9%)相当.Ⅱ类化合物体外对L1210细胞及体内对荷艾氏腹水癌小鼠均有一定抗癌活性。
In this paper, we designed and synthesized 18 compounds of 2- (E) -substituted benzylidenecyclopentanone (Ⅰ) and 11 compounds of Mannich base hydrochloride (Ⅱ), of which 22 were new compounds. The preliminary pharmacological results showed that: for carrageenan-induced rat’s toe edema, Ⅰ_4, Ⅰ_ (12) and Ⅰ_ (13) oral administration of a more significant inhibitory effect, subcutaneous injection of water-soluble compounds have a strong inhibitory effect , Of which the inhibitory rates of Ⅱ_3 at doses of 50, 25 and 12.5 mg / kg were 95.8%, 70.3% and 44.2%, respectively, which were comparable to those of ibuprofen (25 mg / bg inhibition 72.9%). L1210 cells and in vivo Hoechst ascites cancer mice have a certain anti-cancer activity.