Functional foldamers that target bacterial membranes: The effect of charge, amphiphilicity and conformation.

Bioorg Med Chem

School of Pharmacy and Biomedical Sciences, University of Central Lancashire, Preston PR1 2HE, UK. Electronic address:

Published: September 2016

By varying the molecular charge, shape and amphiphilicity of a series of conformationally distinct diarylureas it is possible to control the levels of phospholipid membrane lysis using membranes composed of bacterial lipid extracts. From the data obtained, it appears as though the lysis activity observed is not due to charge, conformation or amphiphilicity in isolation, but that surface aggregation, H-bonding and other factors may also play a part. The work provides evidence that this class of foldamer possesses potential for optimisation into new antibacterial agents.

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http://dx.doi.org/10.1016/j.bmc.2016.07.017DOI Listing

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