Synthesis and biological evaluation of new N-linked 5-triazolylmethyl oxazolidinones
Synthesis and biological evaluation of new N-linked 5-triazolylmethyl oxazolidinones
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新型N-连接5-三唑基甲基恶唑烷酮的合成和生物学评价。
DOI：
10.1016/j.ejmech.2007.09.010
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发表时间：
2008-08-01
影响因子：
6.7
通讯作者：
Yang, Yushe
中科院分区：
文献类型：
--
作者：
Fan, Houxing;Chen, Yilang;Yang, Yushe
合成了一系列新的含N-连接的5-三唑基甲基的恶唑烷酮类化合物，并对其体外抗菌活性（MIC）进行了评价。该系列中的一些类似物显示出优于利奈唑胺和万古霉素的活性上级。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;所选化合物显示出合理的生物利用度以及与利奈唑胺相当的体内功效。(c)2007年Elsevier Masson SAS。All rights reserved.
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. (c) 2007 Elsevier Masson SAS. All rights reserved.