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Letters in Drug Design & Discovery

Author(s): Xiudong Ding, Zhanfeng Gao, Siyu Liu, Sicong Xu, Zhiwei Li, Jia Jiang, Ruixi Fan, Tong Chen, Yanfang Zhao, Hengzhi Lu* and Yunlei Hou*

DOI: 10.2174/1570180820666230118124058

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

Page: [928 - 937] Pages: 10

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Abstract

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 μg/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.

Keywords: Oxazolidinone derivatives, dithiocarbamate moiety, antibacterial activities, Gram-positive bacteria, drug design, drug synthesis.

Graphical Abstract

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