Synthesis and antibacterial activity evaluation of novel biaryloxazolidinone analogues containing a hydrazone moiety as promising antibacterial agents

被引：35

作者：

Wu, Yachuang ^{[1
]}

Ding, Xiudong ^{[2
]}

Ding, Liang ^{[1
]}

Zhang, Yongsheng ^{[1
]}

Cui, Lei ^{[2
]}

Sun, Lu ^{[1
]}

Li, Wei ^{[1
]}

Wang, Di ^{[2
]}

Zhao, Yanfang ^{[1
]}

机构：

[1] Shenyang Pharmaceut Univ, Key Lab Struct Based Drug Design & Discovery, Minist Educ, 103 Wenhua Rd, Shenyang 110016, Liaoning, Peoples R China

[2] 309th Hosp Chinese Peoples Liberat Army, Dept Clin Lab, Beijing 100091, Peoples R China

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2018年 / 158卷

关键词：

Biaryloxazolidinone; Hydrazone moiety; Antibacterial activity; Gram-positive organisms; GRAM-POSITIVE INFECTIONS; STAPHYLOCOCCUS-AUREUS; DESIGN; RESISTANCE; ANTIBIOTICS; DERIVATIVES;

D O I：

10.1016/j.ejmech.2018.09.004

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of linezolid analogues containing a hydrazone moiety were designed, synthesized and evaluated for their antibacterial activity. Most compounds exhibited more potent antibacterial activity against S.aureus, MRSA, MSSA, LREF and VRE pathogens as compared with linezolid and radezolid. Compounds 9a, 9c, 9f, 9g, 10m and 10t were more potent against tested clinical isolates of MRSA, MSSA, VRE and LREF as compared to linezolid. Compound 9a exhibited comparable activity with linezolid against human MAO-A for safety evaluation and showed moderate metabolism in human liver microsome. The most promising compound 9a showed remarkable antibacterial activity against S.aureus, MRSA, MSSA, LREF and VRE pathogens with MIC value of 0.0675 mg/mL, respectively, which was 15- to 30-fold more potent than linezolid. (C) 2018 Elsevier Masson SAS. All rights reserved.

引用

页码：247 / 258

页数：12

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