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. 2009 Oct;62(10):539-44.
doi: 10.1038/ja.2009.66. Epub 2009 Jul 24.

Synthesis and combinational antibacterial study of 5''-modified neomycin

Jianjun Zhang  1 , Katherine Keller, Jon Y Takemoto, Mekki Bensaci, Anthony Litke, Przemyslaw Greg Czyryca, Cheng-Wei Tom Chang
Affiliations

Synthesis and combinational antibacterial study of 5''-modified neomycin

Jianjun Zhang et al. J Antibiot (Tokyo). 2009 Oct.

Abstract

A library of 5''-modified neomycin derivatives were synthesized for an antibacterial structure-activity optimization strategy. Two leads exhibited prominent activity against both methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant enterococci (VRE). Antibacterial activities were measured when combined with other clinically used antibiotics. Significant synergistic activities were observed, which may lead to the development of novel therapeutic practices in the battle against infectious bacteria.

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Figures

Figure 1
Figure 1
QSAR Analysis for MIC's from Aminoglycoside Susceptible Strains
Figure 2
Figure 2
QSAR Analysis for MIC's from Aminoglycoside Resistant Strains
Figure 3
Figure 3
Hemolysis of 4e and 4f
Scheme 1
Scheme 1
Synthesis of Neomycin Derivatives
See this image and copyright information in PMC

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