During the past decade, boronic acid derivatives have attracted much attention for their potential in drug discovery and chemical biology. This renaissance is due, in significant part, to the successful development and marketing of antifungal and antibacterial benzoxaborole derivatives. Yet many questions remain unanswered regarding the physical properties and stability of the benzoxaborole ring and other related boron heterocycles in aqueous media. Likewise, more studies are needed to gain a detailed understanding of the interactions of boron heterocycles with biomolecules to realize their full potential as drug candidates. In this presentation some of these questions will be addressed, and new boron heterocycles will be described along with an evaluation of their suitability toward uses that require aqueous conditions. In this regard, the design and application of stable boronic esters in the fast bioorthogonal conjugation of proteins will also be discussed.

Boron heterocycles: Studies on their properties and applications in drug discovery and chemical biology

255th National Meeting (2018)

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