二苯甲基哌嗪类化合物的合成及其抗变态反应活性  

Synthesis and antiallergic activities of diphenylmethylpiperazine derivatives

作　　者：王立升[1] 姜红宇[1] 周永红[1] 刘百里[2] 计志忠[2] 

机构地区：[1]广西大学工业测试实验中心,广西南宁530004 [2]沈阳药科大学制药工程学院,辽宁沈阳110016

出　　处：《中国药物化学杂志》2002年第3期125-129,共5页Chinese Journal of Medicinal Chemistry

摘　　要：目的设计并合成二苯甲基哌嗪类化合物 ,寻找高活性抗变态反应化合物。方法采用化学合成方法合成所设计的目标化合物 ,并经元素分析、核磁共振氢谱及红外光谱确证其化学结构。采用2 ,4 二硝基氯苯 (DNCB)诱导的小鼠接触性皮炎和组胺致小鼠毛细血管通透性增加两种药理试验模型对部分目标化合物进行了活性测定。结果共合成了 2 1个目标化合物 ,其中 17个化合物未见文献报道。药理实验结果表明 :WLS0 4和WLS11具有较强的抗变态反应活性 ,WLS10 ,WLS11,WLS12 ,WLS17和WLS18具有较强的抗组胺活性。结论随着碳链的增长 ,抗变态反应活性增强 。Aim To design and synthesize diphenylmethylpiperazine derivatives and find high antiallergic compounds.Methods Chemical synthetic methods were used to synthesize these target compounds which were identified by IR, 1H NMR spectral and elemental analysis.Some compounds were evaluated from two pharmacological models of the delayed type hypersensitivity response to DNCB in mice and vascular permeability reduced by histamine in mice.Results Twenty one target compounds were synthesized and seventeen of them had not been found in literature.The pharmacological results showed that WLS04 and WLS11 had high antiallergic effects on the delayed type hypersensitivity,WLS10,WLS11,WLS12,WLS17 and WLS18 had high antihistamic activity.Conclusion Antiallergic activities were getting stronger along with getting longer on the carbon chain.This accorded with the designing idea.

关 键 词：二苯甲基哌嗪类衍生物 抗变态 抗组胺 

分 类 号：R914[医药卫生—药物化学]