Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 51, Issue 19, Pages 6160-6164Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm800345u
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Funding
- National Sciences and Engineering Research Council of Canada (NSERC)
- University of Manitoba
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Aminoglycoside antibiotics and cationic detergents constitute two classes of clinically important drugs and antiseptics. Their bacteriological and clinical efficacy, however, has decreased recently due to antibiotic resistance. We have synthesized aminoglycoside-lipid conjugates in which the aminoglycoside neomycin forms the cationic headgroup of a polycationic detergent. Our results show that neomycin-C-16 and neomycin-C-20 conjugates exhibit strong Gram-positive activity but reduced Gram-negative activity. The MIC of neomycin-C-16 (C-20) conjugates against methicillin-resistant Staphylococcus aureus (MRSA) is comparable to clinically used antiseptics.
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