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

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.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Wu Y,Ding X,Ding L,Zhang Y,Cui L,Sun L,Li W,Wang D,Zhao Y

doi

10.1016/j.ejmech.2018.09.004

subject

Has Abstract

pub_date

2018-10-05 00:00:00

pages

247-258

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(18)30778-5

journal_volume

158

pub_type

杂志文章

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