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

被引:28
作者
Jang, SY
Ha, YH
Ko, SW
Lee, W [1 ]
Lee, J
Kim, S
Kim, YW
Lee, WK [1 ]
Ha, HJ
机构
[1] Seoul Natl Univ, Imagene Co Ltd, Biotechnol Incubating Ctr, Seoul 151742, South Korea
[2] Seoul Natl Univ, Ctr ARS Network, Coll Pharm, Seoul 151741, South Korea
[3] Sogang Univ, Dept Chem, Seoul 121742, South Korea
[4] Hankuk Univ Foreign Studies, Dept Chem, Yongin 449791, South Korea
关键词
antibacterial; oxazolidinone; thioamide;
D O I
10.1016/j.bmcl.2004.05.066
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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. (C) 2004 Elsevier Ltd. All rights reserved.
引用
收藏
页码:3881 / 3883
页数:3
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