Synthesis and preliminary antibacterial evaluation of Linezolid-like 1,2,4-oxadiazole derivatives

In the present study the synthesis of new Linezolid-like molecules has been achieved by substitution of the oxazolidinone central heterocyclic moiety with a 1,2,4-oxadiazole ring. Two series of 1,2,4-oxadiazoles, bearing different side-chains and containing a varying number of fluorine atoms, were synthesized and preliminarily tested for biological activity against some Gram-positive and Gram-negative bacteria using Linezolid and Ceftriaxone as reference drugs.

Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slideHighlights► Two series of 1,2,4-oxadiazoles analogues of Linezolid were synthesized. ► The sequence of the synthetic steps was crucial to obtain title compounds. ► Obtained compounds were tested to evaluate their antibacterial activity.