• Title/Summary/Keyword: Oxazolidinone

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Synthesis of Oxazolidinone Phosphonate Derivatives, Part I

  • Hwang, Jae-Min;Shin, Woon-Seob;Jung, Kang-Yeoun
    • Bulletin of the Korean Chemical Society
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    • v.25 no.9
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    • pp.1326-1330
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    • 2004
  • Several new derivatives of oxazolidinone phosphonate, that are expected to show biological activity, were prepared efficiently by previously published methods. ${\gamma}$-Ketophosphonate 1 was synthesized using pentacovalent oxaphosphorane chemistry followed by reductive amination with aromatic amine of oxazolidinone 4. Biological activity of the synthetic compounds has been studied. One of the synthetic compounds showed promising result for us to pursue further studies.

Synthesis of N-[2-(3,5-dimethyl-4-methoxypyridyl)alkyl]oxazolidinone Analogues and Evaluation of their Proton Pump Enzyme Inhibitions (N-[2-(3,5-디메틸-4-메톡시피리딜)알킬]옥사졸리디논 유도체의 합성 및 프로톤 펌프 효소 저해 효과)

  • Yoon, Sung-Hwa;Kim, Do-Young;Hwang, Sung-Kwan
    • YAKHAK HOEJI
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    • v.41 no.2
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    • pp.174-180
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    • 1997
  • Four oxazolidinone analogues(6, 7, 8, 9), which are isosters of 5, were synthesized by the reaction of 2-chloroalkyl-3,5-dimethyl-4-methoxypyridine with the corresponding benzox azolidinone or oxazolidinone, respectively, and were evaluated for their inhibitory activities toward proton pump enzyme under in vitro condition. Isosteric substitution of the benzothiazolidine moiety in 5 with benzoxazolidinone rendered the molecule relatively inactive.

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Synthesis of Oxazolidinone Phosphonate Derivatives, Part II

  • Hwang, Jae-Min;Yeom, Sung-Ho;Jung, Kang-Yeoun
    • Bulletin of the Korean Chemical Society
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    • v.28 no.5
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    • pp.821-826
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    • 2007
  • Several oxazolidinones, a new class of synthetic antibacterial agents, have shown biological activity against multidrug-resistant gram positive organisms such as staphylococci, streptococci, and enterococci. Previous results of our studies with benzoxazolidinone phosphonate derivatives have demonstrated very low antibacterial activity. In the course of our studies directed towards the discovery of noble antibacterial agents, we have synthesized several new derivatives of oxazolidinone phosphonates prepared efficiently from commercially available amino acids. These compounds are tested for in vitro antibacterial activity and one of the compounds showed promising results allowing us to pursue further studies.

Synthesis and In Vitro Antibacterial Activity of Quaternary Ammonium Cephalosporin Derivatives Bearing Oxazolidinone Moiety

  • Chung, In-Hwa;Kim, Choong-Sup;Seo , Jae-Hong;Chung, Bong-Young
    • Archives of Pharmacal Research
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    • v.22 no.6
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    • pp.579-584
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    • 1999
  • Several oxazolidinones having amine moiety were prepared to form a quaternay ammonium salt with cephalosporin nucleus, and antibacterial activity of the quaternary ammonium cephalosporin derivatives bearing oxazolidinone moiety were examined particularly with expectation of dual activity. However, the cephalosporin-oxazolidinone compounds revealed rather weaker antibacterial activity in vitro than their parent oxazolidinone and cephalosporin without showing any characteristic activity as expected.

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Synthesis, Crystal Structure and Fungicidal Activities of New Type Oxazolidinone-Based Strobilurin Analogues

  • Li, Yuhao;Liu, Rui;Yan, Zhangwei;Zhang, Xiangning;Zhu, Hongjun
    • Bulletin of the Korean Chemical Society
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    • v.31 no.11
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    • pp.3341-3347
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    • 2010
  • A series of oxazolidinone-based strobilurin analogues were efficiently synthesized by the reaction of 3-(2-bromomethylphenyl) oxazolidin-2-one with 1-substituted phenyl-2H-pyrazolin-3-one. Their structures were confirmed and characterized by $^1H$-NMR, $^{13}C$-NMR, elemental analysis, and mass spectroscopy. In addition, the crystal structure of the target compound 3-(2-((1-phenyl-2H-pyrazol-3-yloxy)methyl)phenyl) oxazolidin-2-one was determined by single crystal X-ray diffraction. The bioassay results of these compounds indicated that some of the oxazolidin-2-one derivatives containing N-substituted phenyl 2H-pyrazol ring exhibited potential in vivo fungicidal activities against M. grisea at the dosage of $1\;g\;L^{-1}$.