Synthesis and Biological Evaluation of Novel Oxazolidinone Derivatives Containing Dithiocarbamate Moiety as Antibacterial Agents

被引:0
|
作者
Ding, Xiudong [1 ]
Gao, Zhanfeng [2 ]
Liu, Siyu [2 ]
Xu, Sicong [2 ]
Li, Zhiwei [2 ]
Jiang, Jia [2 ]
Fan, Ruixi [2 ]
Chen, Tong [2 ]
Zhao, Yanfang [2 ]
Lu, Hengzhi [1 ,3 ]
Hou, Yunlei [2 ]
机构
[1] Peoples Liberat Army Gen Hosp, Eighth Med Ctr, Dept Clin Lab, Beijing 100091, Peoples R China
[2] Shenyang Pharmaceut Univ, Sch Pharmaceut Engn, 103 Wenhua Rd, Shenyang 110016, Peoples R China
[3] Peoples Liberat Army Gen Hosp, Med Ctr 8, Dept Clin Lab, Beijing 100091, Peoples R China
关键词
Oxazolidinone derivatives; dithiocarbamate moiety; antibacterial activities; Gram-positive bacteria; drug design; drug synthesis; RESISTANCE;
D O I
10.2174/1570180820666230118124058
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Background In this article, a series of novel oxazolidinone derivatives containing dithiocarbamate moieties have been designed and synthesized.Materials and Methods Their antibacterial activities were measured against Staphylococcus aureus, vancomycin-resistant Enterococcus faecium (VREF), linezolid-resistant Enterococcus faecalis (LREF) and Streptococcus agalactiae (GBS) by minimal inhibitory concentration (MIC) assays.Results Dithiocarbamates were found conducive to the maintenance of antibacterial activity. Most of them exhibited potent activity against Gram-positive pathogens comparable to linezolid. The most promising compound A8 showed remarkable antibacterial activity against S.aureus, VREF, LREF, and GBS pathogens with MIC values between 0.25 and 1 mu g/mL, which might be a promising drug candidate for further investigation.Conclusion A series of novel oxazolidinone derivatives containing dithiocarbamate moieties might be promising drug candidates for further investigation.
引用
收藏
页码:928 / 937
页数:10
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