›› 2017, Vol. 39 ›› Issue (2): 149-158.doi: 10.16507/j.issn.1006-6055.2017.03.008

• 科技态势与趋势 • 上一篇    下一篇

作用于酶的含哌嗪化合物研究进展

甘淋玲1,2  陈永洁2  张亚红1   

  1.  1. 重庆医药高等专科学校,重庆401331 ; 2. 重庆医科大学药学院,重庆400016
  • 收稿日期:2016-08-16 修回日期:2016-09-27 出版日期:2017-04-25 发布日期:2017-04-26
  • 基金资助:

    重庆市科技项目( cstc2016jcyjA0437) ,重庆医药高等专科学校科研项目( ygz2013108) 资助

Research Advances of Piperazine Containing Compounds Targeting Enzymes

GAN Linling1,2 CHEN Yongjie2 ZHANG Yahong1   

  1. 1. Chongqing Medical and Pharmaceutical College,Chongqing 401331,China;
    2.School of Pharmaceutical Sciences,Chongqing Medical University,Chongqing 400016,China
  • Received:2016-08-16 Revised:2016-09-27 Online:2017-04-25 Published:2017-04-26

摘要:

哌嗪环是药物结构修饰中常用的一类重要氮杂环,在以DNA 拓扑异构酶、羊毛甾醇14α-去甲基化酶、( 1,3) -β-D-葡聚糖合成酶、11β -羟基固醇脱氢酶1、葡萄糖激酶、β-分泌酶和脂肪酰胺水解酶等为靶点的化合物中引入哌嗪环,不仅可以增强药物疗效,改善药物的药代动力学性质,而且易被其他官能团修饰,构成多药理靶点的杂合体,呈现出广泛的生物活性,可用于治疗细菌感染、真菌感染、2 型糖尿病、阿尔茨海默病以及疼痛等,具有很大的开发价值。本文综述了作用于酶的含哌嗪化合物在抗菌、抗真菌、抗糖尿病、治疗阿尔茨海默病与镇痛等方面的最新进展及其构效关系。

关键词: 哌嗪, 抗菌, 抗真菌, 抗糖尿病, 抗阿尔茨海默病, 镇痛, 脂肪酰胺水解酶抑制剂

Abstract:

Piperazine ring is an important class of heterocyclic nitrogen which is widely used in structural modification of drugs.The introduction of piperazine ring into compounds,which are targeting DNA topoisomerase,lansterol 14α-demethylase,(1,3) -β-D-glucan synthase,11β-hydroxy steroid dehydrogenase 1,glucokinase,beta-site APP cleaving enzyme 1 and fatty acid amide hydrolase,not only could enhance their efficacy and improve pharmacokinetic properties,but also could be easy to be modified to constitute a hybrid with multi pharmacological targets. These compounds have shown a wide range of biological activities and could be used for the treatment of bacterial infection,fungal infection,type 2 diabetes,Alzheimer's disease and pain,which have great development value.Therefore,the recent advances of the piperazine-containing compounds as antibacterial agents,antifungal agents,anti-diabetes agents,anti-Alzheimer's disease agents and anodyne were described,and their structure-activity relationship were also reviewed.

Key words: piperazine, antibacterial, antifungal, anti-diabetes, anti-Alzheimer's disease, analgesia, FAAH inhibitor

中图分类号: