Synthesis and in vitro biological evaluation of aryl boronic acids as potential inhibitors of factor XIa

A series of functionalized aryl boronic acids were synthesized and evaluated as potential inhibitors of factor XIa. Crystal structures of the protein–inhibitor complexes led to the design and synthesis of second generation compounds showing single digit micromolar inhibition against FXIa and selectivity against thrombin, trypsin, and FXa.

Graphical abstractA series of functionalized aryl boronic acids were synthesized and evaluated as potential inhibitors of factor XIa. Several of the compounds show a single digit micromolar inhibition against FXIa and selectivity against thrombin, trypsin, and FXa.Figure optionsDownload full-size imageDownload as PowerPoint slide