• Title/Summary/Keyword: 2-Oxazolidinone

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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, 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 $1\;g\;L^{-1}$.

Antimicrobial Activities of LCB01-0183, a New Oxazolidinone (새로운 옥사졸리디논계 항균제 LCB01-0183의 항균 활성)

  • Lee, Hyun-Hee;Jung, Sung-Ji;Jeong, Ji-Woong;Cho, Young-Lag;Kim, Yong-Zu;Kwak, Jin-Hwan
    • YAKHAK HOEJI
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    • v.57 no.2
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    • pp.95-100
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    • 2013
  • This study was performed to analyze in vitro and in vivo activities of LCB01-0183, a new oxazolidinone, against clinical isolates of bacteria. In vitro antibacterial activity of LCB01-0183 was tested by the two fold agar dilution method. In vivo activity of LCB01-0183 was determined against systemic infections in mice. LCB01-0183 showed most potent activity among the test compounds against clinical isolates of Gram-positive bacteria. Furthermore, the protective activity of LCB01-0183 was very effective against systemic infections in mice by oral or subcutaneous administration. In time kill study, LCB01-0183 showed a bacteriostatic activity during 24 hours. LCB01-0183 had potent in vitro and in vivo activity against Gram-positive bacteria including drug-resistant strains.

A Facile Synthetic Method of 2-Oxaxolidinones and 1,3-Oxazine-2-ones, Essential Moieties of New Antiulcer Agent

  • Park, Min-Soo;Lee, Jae-Won
    • Archives of Pharmacal Research
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    • v.16 no.2
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    • pp.158-160
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    • 1993
  • 2-Oxazolidinones and 1,3-oxazine-2-ones, key moieties of new antiulcer agents, were prepared successfully by treating corresponding hydroxyamide with N-bromosuccinimide (NBS) and silveracetate in acetonitrile. From the fact that the methods for the preparation of hydoxy amides are versatile and such amides could be converted to the corresponding 2-oxazolid-iones and 1,3-oxazine-2-one under our reaction condition, we think that our method is very practical one for the preparation of such compounds. In addition, the above synthetic example affords a good evidence of the synthetic applicability of our improved Hofmann rearrangement.

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High-Quality Whole Genome Sequence of a Linezolid-Resistant and Vancomycin-Susceptible Enterococcus faecalis Isolate ES-2-1 from a Pig Stool in South Korea

  • Jun Bong Lee;Nguyen Thi Mai Tho;Se Kye Kim;Jang Won Yoon
    • Microbiology and Biotechnology Letters
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    • v.52 no.1
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    • pp.88-90
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    • 2024
  • We report the whole genome sequence of a linezolid-resistant and vancomycin-susceptible Enterococcus faecalis strain, ES-2-1, which was isolated from a pig stool in South Korea. The assembled genome of ES-2-1 consists of a 2,648,168-bp circular chromosome containing the optrA gene (encoding the ABC-F type ribosomal protection protein), an 84,891-bp plasmid containing numerous antimicrobial resistance genes, and an 82,106-bp cryptic plasmid. The ES-2-1 strain belongs to sequence type 1024 (ST1024) and carries multidrug resistant genes including the optrA (oxazolidinone phenicol transferable resistance A) gene, which confers linezolid resistance.