Invasive fungal infections have become an important healthcare issue due in large part to high mortality rates under standard of care (SOC) therapies, creating an urgent need for new and effective anti-fungal agents. We have discovered a series of non-peptide, structurally-constrained analogs of host defense proteins that have distinct advantages over peptides for pharmaceutical use. In this poster we report the chemical optimization of bis-guanidine containing analogs focused on alterations of the central aryl core and the connection of it to the terminal guanidines. This effort has resulted in the production of highly potent, broadly active compounds with low mammalian cell cytotoxicity that have comparable or improved antifungal activities over SOC agents. One representative compound, shown below, was also found to possess favorable <i>in vitro</i> pharmaceutical and off-target properties potentially suitable for further development.

Highly potent, broadly active antifungal agents for the treatment of invasive fungal infections

ACS Fall 2021

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