Antibiotic resistant bacterial infections represent a growing obstacle in clinical treatment, extending hospital stays and contributing to increased mortality. As such, developing and identifying novel antimicrobials effective against these resistant strains is of great importance. Solid phase combinatorial synthesis allows for the rapid production of thousands of potential antimicrobial compounds. In compliment to this mode of synthesis, our previous work presented a high throughput screening method as a means to rapidly identify potent antimicrobial peptoids against E. coli. Work to be discussed here focuses on the optimization of combinatorial peptoid library design through a quantitative study of how peptoid lipophilicity relates to antibacterial potency and mammalian cell toxicity. The information gleaned from this optimization was then applied using the aformentioned screening method to examine the relative potency of peptoid libraries against A. baumanii, E. faecalis, and S. aureus prior to and following lipophilic functionalization.

Evaluating the effect of lipophilicity on antimicrobial potency, cytotoxicity, and combinatorial library design

253rd National Meeting (2017)

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