Synthesis and biological evaluation of new N-linked 5-triazolylmethyl oxazolidinones.

Fan H; Chen Y; Jiang Z; Zhang S; Zhong D; Ji R; Yang Y

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Synthesis and biological evaluation of new N-linked 5-triazolylmethyl oxazolidinones.

机译：新型N-连接的5-三唑基甲基恶唑烷酮的合成及生物学评价。

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A new series of oxazolidinones bearing N-linked 5-triazolylmethyl group have been synthesized and their in vitro antibacterial activities (MIC) were evaluated against a spectrum of resistant and susceptible Gram-positive organisms. Some of the analogues in this series displayed activity superior to linezolid and vancomycin. Furthermore, in vivo efficacies and pharmacokinetic properties of the selected compounds were also disclosed herein; the selected compounds showed reasonable bioavailability as well as in vivo efficacy comparable to that of linezolid.

机译：合成了一系列带有N-连接的5-三唑基甲基的恶唑烷酮，并针对一系列耐药和易感的革兰氏阳性生物评估了它们的体外抗菌活性（MIC）。该系列中的某些类似物显示出优于利奈唑胺和万古霉素的活性。此外，本文还公开了所选化合物的体内功效和药代动力学性质。所选择的化合物显示出与利奈唑胺相当的合理生物利用度和体内功效。

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来源
《European Journal of Medicinal Chemistry: Chimie Therapeutique》 |2008年第8期|共9页
作者
Fan H; Chen Y; Jiang Z; Zhang S; Zhong D; Ji R; Yang Y;
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原文格式 PDF
正文语种 eng
中图分类医药、卫生;劳动卫生;
关键词
Synthesis; in vivo; linezolid; Evaluation;

机译：合成;体内;利奈唑胺;评价;

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Synthesis and biological evaluation of new N-linked 5-triazolylmethyl oxazolidinones.

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