Article

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

Medicinal Chemistry, Daiichi Asubio Medical Research Laboratories, LLC, One Kendall Square, Building 700, Cambridge, MA 02139, USA.
Bioorganic & Medicinal Chemistry Letters (impact factor: 2.55). 11/2006; 16(19):5022-7. DOI:10.1016/j.bmcl.2006.07.043 pp.5022-7
Source: PubMed

ABSTRACT 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.

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Keywords

Crystal structures
 
functionalized aryl boronic acids
 
potential inhibitors
 
second generation compounds
 
single digit micromolar inhibition
 
trypsin