Functional foldamers that target bacterial membranes: The effect of charge, amphiphilicity and conformation. Issue 18 (15th September 2016)

• Record Type: Journal Article
• Authors: Patil-Sen, Yogita; Dennison, Sarah R.; Snape, Timothy J.
• Is Part Of: Bioorganic & medicinal chemistry. Volume 24:Issue 18(2016)
• Page Start: 4241
• Page End: 4245
• Publication Date: 2016-09-15
• Subjects: Foldamer -- Antibacterial -- Membrane -- Diarylureas -- Conformation; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; Biochemistry -- Periodicals; Chemistry, Clinical -- Periodicals; Chemistry, Organic -- Periodicals; Chimie bio-organique -- Périodiques; Chimie pharmaceutique -- Périodiques; 615.19
• DOI: 10.1016/j.bmc.2016.07.017
• Languages: English
• ISSNs: 0968-0896

Abstract

Graphical abstract: 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.