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 Gramnegative bacteria using Linezolid and Ceftriaxone as reference drugs.
Palumbo Piccionello, A., Musumeci, R., Cocuzza, C., Fortuna, C.G., Guarcello, A., Pierro, P., et al. (2012). Synthesis and preliminary antibacterial evaluation of Linezolid-like 1,2,4-oxadiazole derivatives. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 50(50), 441-448 [10.1016/j.ejmech.2012.02.002].
Synthesis and preliminary antibacterial evaluation of Linezolid-like 1,2,4-oxadiazole derivatives
PALUMBO PICCIONELLO, Antonio;GUARCELLO, Annalisa;PIERRO, Paola;PACE, Andrea
2012-01-01
Abstract
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 Gramnegative bacteria using Linezolid and Ceftriaxone as reference drugs.
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