Bioorganic & Medicinal Chemistry Letters 2004-08-02

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

Sun-Young Jang, Young Hwan Ha, Seung Whan Ko, Wonku Lee, Jongkook Lee, Sunghoon Kim, Yong Woo Kim, Won Koo Lee, Hyun-Joon Ha

Index: Bioorg. Med. Chem. Lett. 14(15) , 3881-3, (2004)

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Abstract

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.