An Update on the Structure of Oxazolidinone Analogs and a Comparison with Linezolid in Terms of In Vitro and Intracellular Efficacy against Clinically Relevant Bacterial Species

Japanese journal of infectious diseases

Di Wang¹  Qian Tang¹  Boxuan Xu²  Ping Gong²  Yanfang Zhao² 

[1] Department of Clinical Laboratory, The 309th Hospital of Chinese People’s Liberation Army;School of Pharmaceutical Engineering, Shenyang Pharmaceutical University

关键词: oxazolidinone;    antimycobacterial activity;    Gram-positive;    mycobacterium;    Helicobacter pylori;   

DOI  :  10.7883/yoken.JJID.2017.104

学科分类：传染病学

来源: National Institute of Infectious Diseases

【 摘 要 】

Oxazolidinones constitute a novel class of antimicrobials as inhibitors of bacterial ribosomal protein synthesis. In this study, we identified 15 novel oxazolidinone analogs with potent antituberculosis activities. Compounds sy124 and sy125 showed the best activity in vitro (better than that of the linezolid) against various clinically relevant bacterial species, including most Gram-positive bacteria, Mycobacterium spp., and Helicobacter pylori. A cell-based assay indicated that these compounds have a strong ability to kill intracellular pathogens. Our results reveal that the newly identified compounds may be further developed as novel antimicrobial agents.

【 授权许可】

Unknown