Literature DB >> 29525221

3-Hydroxy-1,5-dihydro-2H-pyrrol-2-ones as novel antibacterial scaffolds against methicillin-resistant Staphylococcus aureus.

Alexander Q Cusumano1, Joshua G Pierce2.   

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.
Copyright © 2018 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Antibiotics; Cyclization; Heterocycles; Medicinal chemistry; Natural products

Mesh:

Substances:

Year:  2018        PMID: 29525221      PMCID: PMC6111006          DOI: 10.1016/j.bmcl.2018.02.047

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


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