TY - CONF
T1 - Asymmetric synthesis and biological evaluation of 1,2,4-Oxadiazoles analogues of Linezolid
AU - Palumbo Piccionello, Antonio
AU - Pace, Andrea
AU - Buscemi, Silvestre
AU - Accardo, Angela
AU - Pierro, Paola
PY - 2014
Y1 - 2014
N2 - Oxazolidinones are a class of antibacterial agents which displayed activity againist a variety of gram-positive pathogens and are highly potent against multidrug-resistant bacteria. Linezolid is the first oxazolidinone antibiotic approved for clinical use but linezolid resistance began to appear. 1,2,4 – Oxadiazoles are known bioactive heterocycles whose activity has been often associated to their bioisosterism with amide or ester functionalities [1]. As results of a research project on the molecular design of heterocycle – based antibacterials to contrast Multi-Drug Resistance (MDR) [2], we report the synthesis of 1,2,4 - Oxadiazole analogues of Linezolid. The synthesis has been achieved by substitution of the morpholine ( C-ring ) with the Oxadiazole ring [3,4]. The central oxazolidinone ring was obtained through the Manninen reaction. Synthesized compounds showed good activity against Linezolid-resistant bacteria.
AB - Oxazolidinones are a class of antibacterial agents which displayed activity againist a variety of gram-positive pathogens and are highly potent against multidrug-resistant bacteria. Linezolid is the first oxazolidinone antibiotic approved for clinical use but linezolid resistance began to appear. 1,2,4 – Oxadiazoles are known bioactive heterocycles whose activity has been often associated to their bioisosterism with amide or ester functionalities [1]. As results of a research project on the molecular design of heterocycle – based antibacterials to contrast Multi-Drug Resistance (MDR) [2], we report the synthesis of 1,2,4 - Oxadiazole analogues of Linezolid. The synthesis has been achieved by substitution of the morpholine ( C-ring ) with the Oxadiazole ring [3,4]. The central oxazolidinone ring was obtained through the Manninen reaction. Synthesized compounds showed good activity against Linezolid-resistant bacteria.
UR - http://hdl.handle.net/10447/96917
M3 - Other
SP - 81
EP - 81
ER -