从耐药机制看抗菌药物的发展

Development of Antibiotics Based on Bacterial Resistance

抗菌药物耐药机制包括:(1)靶位修饰;(2)产灭活酶;(3)药物渗透力下降;(4)外排泵表达。本文从增加作用靶位、改善药物与靶位结合力、联合酶抑制药的复方药物、寻找体外泵抑制剂、发现新代合物和新靶位等方面介绍了临床使用的和临床前的新抗菌药物。

Mechanisms of antibiotics resistance includes ： （ 1 ） target site modification; （ 2 ） production of inactive enzymes; （3）decrease of drugs penetrance;（4）expression of efflux pumps. Thisarticle introduces novel antibiotics, clinically using and pre-clinical, based on target site, improvement combinative power between drug and target, composite drugs of antibiotic plus zymase inhibitor, searching efflux pump inhibitor, finding no vel compounds and target sites.