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- W646567365 abstract "Infections due to methicillin-resistant Staphylococcus aureus (MRSA) are associated with a mortality rate of 15 to 60%. The first report of S. aureus resistant to penicillin occurred in 1942. A series of glycopeptides was prepared at Shionogi and displayed good in vitro anti-MRSA activity, with MICs ranging from 0.20 to 6.25 µg/ml. Daptomycin possesses an unusual amino acid, kynurenine. Modifications of this amino acid were attempted on the ketone and anilino groups. These modifications highlighted the importance of this amino acid for antibacterial activity. One of the most effective antibacterial strategies is to disrupt the integrity of bacterial cell wall formation. Peptidoglycan includes four steps in which amino acid residues are ligated to uridine-diphospho-N-acetylmuramic acid (UDP-MurNac). Benzylidene rhodamine is an inhibitor of MurC and is active against MRSA (MICs, 31 µM). A series of derivatives was synthesized, with the aim of improving logP and water solubility, as well as protein binding. Molecular iron is an essential factor for bacterial growth, iron being used during respiration, DNA replication, and other biological processes. One of the targets of a research was to improve water solubility, to obtain in vivo activity against MRSA, and to obtain both anti-MRSA activity and activity against gram-negative bacteria, including Pseudomonas aeruginosa. Deformylase is an essential bacterial metallo-enzyme responsible for the removal of the N-terminal formyl group from methionine following protein synthesis. Methionine aminopeptidases play a pivotal role in protein biosynthesis." @default.
- W646567365 created "2016-06-24" @default.
- W646567365 creator A5059999356 @default.
- W646567365 date "2014-04-30" @default.
- W646567365 modified "2023-09-25" @default.
- W646567365 title "Agents against Methicillin-Resistant Staphylococcus aureus" @default.
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