AureoGen, Inc.

There is currently an immediate unmet need for new and better drugs to treat of systemic fungal infections.The natural product aureobasidin A (AbA) is a well-tolerated antifungal agent with robust efficacy in animals and a mode of action that is distinct from all drugs in current clin. use.However, although native AbA is active, and quite potent, against essentially all yeasts, as well a number of other fungi, it has little activity against the filamentous fungus Aspergillus fumigatus.A.fumigatus is an important human pathogen and attempts to improve AbA′s activity this organism, by structural modifications, have to date involved chemistries too complex and costly for continued development.AureoGen has developed an entirely new, and much simpler, approach to modify the structure of AbA.The key step in the chem. involves functionalization of the phenylalanine residues in the compound by iridium-catalyzed borylation.This is followed by displacement of the pinacol boron moiety to form the corresponding bromide or iodide and substitution by Suzuki biaryl coupling.The chem. allows for synthesis of a truly wide range of derivatives and has to date produced compounds with A.fumigatus minimal inhibitory concentrations of < 0.12 μg/mL.The approach is also readily adaptable to large-scale synthesis and industrial production