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.
Accardo, A., PALUMBO PICCIONELLO, A., Pace, A., Pierro, P., Buscemi, S., Fortuna, C., et al. (2014). Asymmetric synthesis and biological evaluation of 1,2,4-Oxadiazoles analogues of Linezolid. In 14th Anglo-Italian Meeting on Heterocyclic Chemistry (pp.81-81).
Autori: | Accardo, A.; PALUMBO PICCIONELLO, A.; Pace, A.; Pierro, P.; Buscemi, S.; Fortuna, C.; Musumeci, R. | |
Titolo: | Asymmetric synthesis and biological evaluation of 1,2,4-Oxadiazoles analogues of Linezolid | |
Settore Scientifico Disciplinare: | Settore CHIM/06 - Chimica Organica | |
Data di creazione: | 2014 | |
Nome del convegno: | 14th Anglo-Italian Meeting on Heterocyclic Chemistry | |
Luogo del convegno: | Windsor, UK | |
Anno del convegno: | 29 Giugno-1 Lluglio 2014 | |
Data di concessione: | 2014 | |
Data di pubblicazione: | 2014 | |
Numero di pagine: | 1 | |
Citazione: | Accardo, A., PALUMBO PICCIONELLO, A., Pace, A., Pierro, P., Buscemi, S., Fortuna, C., et al. (2014). Asymmetric synthesis and biological evaluation of 1,2,4-Oxadiazoles analogues of Linezolid. In 14th Anglo-Italian Meeting on Heterocyclic Chemistry (pp.81-81). | |
Tipologia: | 0 - Proceedings (TIPOLOGIA NON ATTIVA) | |
Appare nelle tipologie: | 0 - Proceedings (TIPOLOGIA NON ATTIVA) |
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