Synthesis and antibacterial evaluation of novel oxazolidinone derivatives containing a piperidinyl moiety

Bioorg Med Chem Lett. 2019 Dec 1;29(23):126746. doi: 10.1016/j.bmcl.2019.126746.

Yunlei Hou ¹, Yuhong Dong ¹, Tianyu Ye ¹, Jia Jiang ¹, Liang Ding ¹, Mingze Qin ¹, Xiudong Ding ², Yanfang Zhao ³

Affiliations

1 School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenhe District, Shenyang 110016, PR China.
2 Department of Clinical Laboratory, The 309th Hospital of Chinese People's Liberation Army, Beijing 100091, China. Electronic address: [email protected].
3 School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenhe District, Shenyang 110016, PR China. Electronic address: [email protected].

PMID: 31676225 DOI: 10.1016/j.bmcl.2019.126746

Abstract

In this article, a series of novel Oxazolidinone derivatives containing a piperidinyl moiety was designed and synthesized. Their Antibacterial activities were measured against S. aureus, MRSA, MSSA, LREF and VRE by MIC assay. Most of them exhibited potent activity against Gram-positive pathogens comparable to linezolid. Among them, compound 9h exhibited comparable activity with linezolid against human MAO-A for safety evaluation and showed moderate metabolism in human liver microsome. The most promising compound 9h, which showed remarkable Antibacterial activity against S. aureus, MRSA, MSSA, LREF and VRE pathogens with MIC value of 0.25-1 μg/mL, was an interesting candidate for further investigation.

Keywords

Antibacterial activities; Linezolid; Oxazolidinone derivatives; Piperidinyl moiety.

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