Design, synthesis, and antibacterial evaluation of a novel series of biaryloxazolidinone derivatives against Gram-positive bacteria

被引：3

作者：

Qi, Yinliang ^{[1
]}

Ding, Xiudong ^{[2
]}

Wang, Kun ^{[1
]}

Yan, Pingzhen ^{[1
]}

Guo, Xinxin ^{[1
]}

Ma, Shiwei ^{[1
]}

Xiao, Mingfei ^{[1
]}

Sun, Pengrui ^{[2
]}

Liu, Siyu ^{[1
]}

Hou, Yunlei ^{[1
]}

Zhao, Yanfang ^{[1
]}

机构：

[1] Shenyang Pharmaceut Univ, Sch Pharmaceut Engn, 103 Wenhua Rd, Shenyang 110016, Liaoning, Peoples R China

[2] Peoples Liberat Army Gen Hosp, Dept Clin Lab, Med Ctr 8, Beijing 100091, Peoples R China

来源：

NEW JOURNAL OF CHEMISTRY | 2022年 / 46卷 / 19期

关键词：

STAPHYLOCOCCUS-AUREUS; OXAZOLIDINONE ANTIBACTERIALS; IN-VITRO; AGENTS; IDENTIFICATION; ANTIBIOTICS; RESISTANCE; DISCOVERY; SAFETY; VIVO;

D O I：

10.1039/d2nj00479h

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

A series of new biaryloxazolidinone derivatives has been designed and synthesized using the combination principle and blocking metabolic site to improve their antibacterial activity and stability. Apart from the excellent antibacterial profile against S. aureus (MIC = 0.25 mu g mL(-1)), MRSA (MIC = 0.25 mu g mL(-1)), LREF (MIC = 0.031 mu g mL(-1)), VRE (MIC = 0.031 mu g mL(-1)), GBS (MIC = 0.031 mu g mL(-1)), and Spn (MIC = 0.031 mu g mL(-1)), compound 13b-6 also displayed good stability and safety, excellent rat PK profile with long half-life time (T-1/2 = 17.7 h), and moderate plasma exposure (AUC(0-t) = 74.4 ng mL(-1)).

引用

页码：9470 / 9485

页数：16

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