2. Academic Validation
  3. Synthesis and antibacterial activity evaluation of novel biaryloxazolidinone analogues containing a hydrazone moiety as promising antibacterial agents

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

  • Eur J Med Chem. 2018 Oct 5:158:247-258. doi: 10.1016/j.ejmech.2018.09.004.
Yachuang Wu 1,  Xiudong Ding 2,  Liang Ding 1,  Yongsheng Zhang 1,  Lei Cui 2,  Lu Sun 1,  Wei Li 1,  Di Wang 3,  Yanfang Zhao 4
Affiliations

Affiliations

  • 1 Key Laboratory of Structure-Based Drug Design and Discovery, Shenyang Pharmaceutical University, Ministry of Education, 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.
  • 3 Department of Clinical Laboratory, The 309th Hospital of Chinese People's Liberation Army, Beijing, 100091, China. Electronic address: wangdi_42869@163.com.
  • 4 Key Laboratory of Structure-Based Drug Design and Discovery, Shenyang Pharmaceutical University, Ministry of Education, 103 Wenhua Road, Shenhe District, Shenyang, 110016, PR China. Electronic address: yanfangzhao@syphu.edu.cn.
PMID: 30218910 DOI: 10.1016/j.ejmech.2018.09.004
Abstract

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.

Keywords

Antibacterial activity; Biaryloxazolidinone; Gram-positive organisms; Hydrazone moiety.

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