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. 2013 Nov:69:779-85.
doi: 10.1016/j.ejmech.2013.09.035. Epub 2013 Sep 25.

Novel promising linezolid analogues: rational design, synthesis and biological evaluation

Margherita De Rosa  1 , Anna Zanfardino, Eugenio Notomista, Thomas A Wichelhaus, Carmela Saturnino, Mario Varcamonti, Annunziata Soriente
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Novel promising linezolid analogues: rational design, synthesis and biological evaluation

Margherita De Rosa et al. Eur J Med Chem. 2013 Nov.

Abstract

A new series of 5-substituted oxazolidinones derived from linezolid, having urea and thiourea moieties at the C-5 side chain of the oxazolidinone ring, were prepared and their in vitro antibacterial activity was evaluated. The compound 10f demonstrated high antimicrobial activity, comparable to that of linezolid against Staphylococcus aureus.

Keywords: Antibacterial; Linezolid; Oxazolidinone; Structure–activity relationship; Thiourea.

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