Download MendeleySynthesis and in vitro biological evaluation of aryl boronic acids as potential inhibitors of factor XIa.
Lazarova, T.I., Jin, L., Rynkiewicz, M., Gorga, J.C., Bibbins, F., Meyers, H.V., Babine, R., Strickler, J.(2006) Bioorg Med Chem Lett 16: 5022-5027
- PubMed: 16876411
- DOI: https://doi.org/10.1016/j.bmcl.2006.07.043
- Primary Citation of Related Structures:
1ZLR, 1ZMJ, 1ZML, 1ZMN - 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.
Organizational Affiliation:
Medicinal Chemistry, Daiichi Asubio Medical Research Laboratories, LLC, One Kendall Square, Building 700, Cambridge, MA 02139, USA. [email protected]
