title: Functional foldamers that target bacterial membranes: The effect of charge, amphiphilicity and conformation.
abstract: 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.
authors.affiliation: School of Pharmacy and Biomedical Sciences, University of Central Lancashire, Preston PR1 2HE, UK.
authors.forename: Yogita
authors.initials: Y
authors.lastname: Patil-Sen
authors.affiliation: School of Pharmacy and Biomedical Sciences, University of Central Lancashire, Preston PR1 2HE, UK.
authors.forename: Sarah R
authors.initials: SR
authors.lastname: Dennison
authors.affiliation: School of Pharmacy and Biomedical Sciences, University of Central Lancashire, Preston PR1 2HE, UK. Electronic address: tjsnape@uclan.ac.uk.
authors.forename: Timothy J
authors.initials: TJ
authors.lastname: Snape
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002462:Cell Membrane / Q000187:drug effects* / Q000378:metabolism; D002463:Cell Membrane Permeability; D004926:Escherichia coli / Q000187:drug effects; D008782:Methylurea Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D008968:Molecular Conformation; D015394:Molecular Structure; D010671:Phenylurea Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D011112:Polymyxin B / Q000494:pharmacology; D013211:Staphylococcus aureus / Q000187:drug effects; D013501:Surface-Active Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000900:Anti-Bacterial Agents; D008782:Methylurea Compounds; D010671:Phenylurea Compounds; D013501:Surface-Active Agents; D011112:Polymyxin B
keywords: Antibacterial; Conformation; Diarylureas; Foldamer; Membrane