The design, synthesis and evaluation of a small series of potent amphiphilic norbornane antibacterial agents has been performed (compound 10 MIC = 0.25 μg/mL against MRSA). Molecular modelling indicates rapid aggregation of this class of antibacterial agent prior to membrane association and insertion. Two fluorescent analogues (compound 29 with 4-amino-naphthalimide and 34 with 4-nitrobenz-2-oxa-1,3-diazole fluorophores) with good activity (MIC = 0.5 μg/mL against MRSA) were also constructed and confocal microscopy studies indicate that the primary site of interaction for this family of compounds is the bacterial membrane.

The challenge with engineering soft materials is to find a chemically functionalized material that can be easily fabricated into complex structures while providing a supportive cellular milieu. The current gold...

No abstract

Convergent, late-stage introduction of premade acylguanidine moieties is a useful strategy for the rapid development of novel compounds containing acylguanidines. As such, robust methodology for suitable acylguanidine building blocks is...