National Center for
1ZMJ: Crystal Structure Of The Catalytic Domain Of Factor Xi In Complex With 4-(guanidinomethyl)-phenylboronic Acid
Synthesis and in vitro biological evaluation of aryl boronic acids as potential inhibitors of factor XIa
Bioorg. Med. Chem. Lett. (2006) 16 p.5022-5027
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.