Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 22, Issue 4, Pages 1499-1503Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.01.025
Keywords
Aminoglycosides; Quaternary ammonium chlorides; Cationic amphiphiles; Huisgen condensation; Phenolic disinfectants
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Funding
- Canadian Institutes of Health Research (CIHR)
- Manitoba Health Research Council (MHRC)
- Natural Sciences and Engineering Research Council of Canada (NSERC)
- Canadian Foundation for Innovation (CFI)
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Here we present a proof-of-concept study, combining two known antimicrobial agents into a hybrid structure in order to develop an emergent cationic detergent-like interaction with the bacterial membrane. Six amphiphilic conjugates were prepared by copper (I)-catalyzed 1,3-dipolar cycloaddition between a neomycin B-derived azide and three alkyne-modified phenolic disinfectants. Three conjugates displayed good activity against a variety of clinically relevant Gram positive and Gram negative bacteria, including MRSA, without the high level of hemolysis or strong binding to serum proteins commonly observed with other cationic antimicrobial peptides and detergents. (C) 2012 Elsevier Ltd. All rights reserved.
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