3-Hydroxy-1,5-dihydro-2H-pyrrol-2-ones as novel antibacterial scaffolds against methicillin-resistant Staphylococcus aureus |
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| Authors: | Alexander Q Cusumano Joshua G Pierce |
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| Institution: | 1. Department of Chemistry, College of Sciences, NC State University, Raleigh, NC 27695, USA;2. Comparative Medicine Institute, NC State University, Raleigh, NC 27695, USA |
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| Abstract: | Herein, we report the synthesis and evaluation of 3-hydroxy-1,5-dihydro-2H-pyrrol-2-ones as antibacterial agents against methicillin-resistant S. aureus (MRSA) and methicillin-resistant S. epidermidis (MRSE). Lead compound 38 showed minimum inhibitory concentrations (MICs) of 8 and 4?μg/mL against MRSA and MRSE, respectively. Furthermore, compound 38 displayed a MIC of 8–16?μg/mL against linezolid-resistant MRSA. These molecules, previously underexplored as antibacterial agents, serve as a new scaffold for antimicrobial development. |
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| Keywords: | Natural products Antibiotics Heterocycles Cyclization Medicinal chemistry |
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