3-Hydroxy-1,5-dihydro-2H-pyrrol-2-ones as novel antibacterial scaffolds against methicillin-resistant Staphylococcus aureus.
Alexander Q Cusumano, Joshua G Pierce
Author Information
Alexander Q Cusumano: Department of Chemistry, College of Sciences, NC State University, Raleigh, NC 27695, USA.
Joshua G Pierce: Department of Chemistry, College of Sciences, NC State University, Raleigh, NC 27695, USA; Comparative Medicine Institute, NC State University, Raleigh, NC 27695, USA. Electronic address: jgpierce@ncsu.edu.
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.
