杂合抗菌药物的研究进展  

Recent Advances in Hybrid Antibacterial Agents

作　　者：陈佳容[1] 邵雷[1] 陈代杰[1,2] 

机构地区：[1]中国医药工业研究总院上海医药工业研究院,创新药物与制药工艺国家重点实验室,上海201203 [2]上海交通大学药学院,上海200240

出　　处：《中国医药工业杂志》2017年第9期1233-1246,共14页Chinese Journal of Pharmaceuticals

基　　金：国家自然基金项目(No.81373310 No.81573329);上海市自然基金项目(No.16ZR1435400)

摘　　要：杂合抗菌药物是一种由2个或多个具有协同效应的抗菌药物或药效基团(活性构件)通过共价连接而成的新型抗菌药物,也包括由抗菌药物与耐药敏化剂(抑制细菌耐药性)共价连接而成的新型抗菌药物,其抗菌效应优于简单的2种分子混合使用。近二十年来,这种新型抗菌药物的研究取得了重要的进展,特别是已有若干个候选药物进入临床研究阶段,展示了这类独特新型抗菌药物的临床应用前景。本文从杂合抗菌药物中不同杂合分子的作用机制的角度进行综述,并简要展望了杂合抗菌药物的发展前景。The hybrid antibacterial agents are a new kind of antibiotics hybridized by covalent linkage of two or more antimicrobial molecules or pharmacophores, or hybridized by covalent linkage of one antimicrobial molecule and the other resistance sensitizing molecule. Great progress has been made in this research field for the discovery of new drugs to combat bacterial resistance over the past two decades. Several candidates of the hybrid antibacterial agents have entered different clinical trial stages, from which show an attractive prospect in further clinical application. In this paper, various hybrid antimicrobials are reviewed according to the mechanisms of their functional entities, and the prospect of hybrid antibacterial agents are also briefly elaborated.

关 键 词：杂合抗菌药物 细菌耐药性 药效基团 耐药敏化剂 

分 类 号：R914[医药卫生—药物化学]