具有N-取代基多样化的芳基哌嗪基恶唑烷酮的合成与抗菌活性
Synthesis and antibacterial activity of arylpiperazinyl oxazolidinones with diversification of the N-substituents.
作者信息
Jang Sun-Young, Ha Young Hwan, Ko Seung Whan, Lee Wonku, Lee Jongkook, Kim Sunghoon, Kim Yong Woo, Lee Won Koo, Ha Hyun-Joon
机构信息
Imagene Co. Ltd, Biotechnology Incubating Center, Seoul National University, Seoul 151-742, South Korea.
出版信息
Bioorg Med Chem Lett. 2004 Aug 2;14(15):3881-3. doi: 10.1016/j.bmcl.2004.05.066.
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.
合成了一系列4-芳基哌嗪-1-基-3-苯基恶唑烷-2-酮衍生物，其N-取代基具有多样性，如亚甲基O-连接杂环、硫代酰胺、二硫代氨基甲酸盐、硫脲和硫代氨基甲酸盐，并作为抗菌剂进行了评估。评估了它们对耐甲氧西林金黄色葡萄球菌（MRSA）和耐万古霉素肠球菌（VRE）等革兰氏阳性耐药菌株（如葡萄球菌和肠球菌）的体外活性（MIC）。大多数化合物在体外比利奈唑胺更有效，但在体内活性较低。
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