噁唑烷酮类抗菌剂构效关系及结构改造研究进展

噁唑烷酮类抗菌药是一类结构类型与作用机制完全不同于目前其他所有抗菌药物的新型合成抗菌药,自首个该类药物利奈唑胺上市后,以获得抗菌谱更广、抗菌活性更高的新型噁唑烷酮类化合物为目标的结构改造方案及有关细菌对化合物耐药机制的研究便全面展开。综述噁唑烷酮类抗菌药的作用机制、构效关系、细菌对其的耐药机制和相关的化合物结构改造的研究进展。

Advances in the Researches on SARs and Structure Modification of Oxazolidinone Antibacterial Agents

The action mechanisms,drug resistance mechanisms,structure-activity relationships (SARs) and structure modification of oxazolidinone antibacterial agents were discussed in this paper.The oxazolidinones antibacterial agents are a promising new class of synthetic antibacterial agents,the structure type and action mechanisms of which were different from those of traditional antibacterial agents.Since the first drug of oxazolidinones,linezolid,was approved by FDA,the researches on resistance mechanisms and vari...