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Chapter 49 : Agents against Methicillin-Resistant

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Abstract:

Infections due to methicillin-resistant (MRSA) are associated with a mortality rate of 15 to 60%. The first report of 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 . 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.

Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49

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Bacterial Proteins
1.0785233
Antibacterial Agents
0.99282664
Chemicals
0.5599055
beta-Lactam Antibiotics
0.54171467
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Figure 81

Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Figure 82

Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Figure 86

Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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Citation: Bryskier A. 2005. Agents against Methicillin-Resistant , p 1183-1238. In Bryskier, M.D. A (ed), Antimicrobial Agents. ASM Press, Washington, DC. doi: 10.1128/9781555815929.ch49
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