Synthesis and antibacterial activity of arylpiperazinyl oxazolidinones with diversification of the N-substituents

Bioorganic & Medicinal Chemistry Letters
Sun-Young JangHyun-Joon Ha

Abstract

A series of 4-arylpiperazin-1-yl-3-phenyloxazolidin-2-one derivatives with diversification of the N-substituents such as methylene O-linked heterocycles, thioamide, dithiocarbamate, thiourea, and thiocarbamate were synthesized and evaluated as antibacterial agents. Their in vitro activities (MIC) were evaluated against MRSA and VRE resistant Gram-positive strains such as Staphylococcus and Enterococcus. Most of the compounds were more potent in vitro but less active in vivo than linezolid.

References

Apr 18, 2002·Bioorganic & Medicinal Chemistry Letters·Du Yu, Guo Huiyuan
Oct 31, 2002·The Journal of Antimicrobial Chemotherapy·Cressida AucklandAlan P Johnson
Nov 5, 2002·European Journal of Clinical Microbiology & Infectious Diseases : Official Publication of the European Society of Clinical Microbiology·A P JohnsonF J Allerberger
Dec 7, 2002·Bioorganic & Medicinal Chemistry·O A PhillipsN Al-Hassawi
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Nov 19, 2003·Bioorganic & Medicinal Chemistry Letters·Michael B GravestockAlan Wookey
Nov 19, 2003·Bioorganic & Medicinal Chemistry Letters·Lisa M ThomascoBetty H Yagi

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Citations

Jul 3, 2013·European Journal of Medicinal Chemistry·Cosimo G FortunaRosario Musumeci
Jan 3, 2006·Bioorganic & Medicinal Chemistry Letters·Braj Bhushan LohrayPrashant Kapadnis

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