两种新型抗自由基药物的合成及抗自由基活性的研究

Synthesis of Two Kinds of New Free Radical Scavengers and Study of Anti-Free Radical Activity

目的 为了提高心血管类药物及结核类药物的抗自由基活性 ,对某些药物作结构修饰 ,以期达到药物与自由基清除剂的双重作用。方法 分别以二苯甲基哌嗪和咖啡酸、儿茶醛和对氨基水杨酸为原料 ,制得 (E) 1 二苯甲基 4 [3 (3,4 二羟苯基 ) 2 丙烯基 ]哌嗪 (I)和儿茶醛缩对氨基水杨酸 (Ⅱ ) ,并通过黄嘌呤 -黄嘌呤氧化酶 -鲁米诺化学发光体系检测其清除O2 · -自由基的活性。结果 合成的两种新化合物经元素分析、红外光谱和核磁共振谱测定 ,与结构相符。化学发光法测定SOD样活性 ,(I)溶液的 [ID]50 为 75 6nmol·L-1;(Ⅱ )溶液的 [ID]50 为 74 5nmol·L-1。结论 新合成的两种化合物不但保留了原药物的有效结构部位 。

Aim To improve anti free radical activities of some cardiovascular and tubercular medicines,structure modification were made so as to attain double functions as medicines and free radical scavengers.Methods Diphenylmethyl piperazine and caffeic acid,catechualyehyde and p aminosalicylic acid were taken as materials respectively to synthesize (E) 1 diphenylmethyl 4 [3 (3,4 dihydroxy phenyl) 2 propenyl] piperazine(I) and Schiff base N catechualyehyde p aminosalicylic acid(Ⅱ).At the same time,scavenging O 2 ·- free radical activities were detected through Xanthine-Xanthine Oxidase Luminol Chemiluminescence system.Results Through elementary analysis and the detection of IR and 'H NMR spectra,results indicated the two new compounds could accord with its constitution.The [ID] 50 values of SOD-like actiuities of solution(I) and solution(Ⅱ) determined by chemiluminesceme were 756 nmol·L -1 and 745nmol·L -1 respectively.Conclusion The two new compounds not only reserve effective structure position of original medicines,but also have strong anti free radical roles.