Literature DB >> 16876411

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

Tsvetelina I Lazarova1, Lei Jin, Michael Rynkiewicz, Joan C Gorga, Frank Bibbins, Harold V Meyers, Robert Babine, James Strickler.   

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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Year:  2006        PMID： 16876411     DOI： 10.1016/j.bmcl.2006.07.043

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  11 in total

1.  A small-molecule factor XIa inhibitor produces antithrombotic efficacy with minimal bleeding time prolongation in rabbits.

Authors:  Pancras C Wong; Earl J Crain; Carol A Watson; William A Schumacher
Journal:  J Thromb Thrombolysis       Date:  2011-08       Impact factor: 2.300

2.  High-resolution crystal structures of factor XIa coagulation factor in complex with nonbasic high-affinity synthetic inhibitors.

Authors:  Xavier Fradera; Bert Kazemier; Emma Carswell; Andrew Cooke; Arthur Oubrie; William Hamilton; Maureen Dempster; Stephan Krapp; Susanna Nagel; Anja Jestel
Journal:  Acta Crystallogr Sect F Struct Biol Cryst Commun       Date:  2012-03-27

Review 3.  Future prospects for contact factors as therapeutic targets.

Authors:  David Gailani
Journal:  Hematology Am Soc Hematol Educ Program       Date:  2014-11-18

Review 4.  Recent advances in the discovery and development of factor XI/XIa inhibitors.

Authors:  Rami A Al-Horani; Daniel K Afosah
Journal:  Med Res Rev       Date:  2018-05-04       Impact factor: 12.944

5.  Discovery of allosteric modulators of factor XIa by targeting hydrophobic domains adjacent to its heparin-binding site.

Authors:  Rajesh Karuturi; Rami A Al-Horani; Shrenik C Mehta; David Gailani; Umesh R Desai
Journal:  J Med Chem       Date:  2013-03-18       Impact factor: 7.446

6.  Sulfated pentagalloylglucoside is a potent, allosteric, and selective inhibitor of factor XIa.

Authors:  Rami A Al-Horani; Pooja Ponnusamy; Akul Y Mehta; David Gailani; Umesh R Desai
Journal:  J Med Chem       Date:  2013-01-28       Impact factor: 7.446

Review 7.  Factor XIa inhibitors: A review of the patent literature.

Authors:  Rami A Al-Horani; Umesh R Desai
Journal:  Expert Opin Ther Pat       Date:  2016       Impact factor: 6.674

Review 8.  Factor XI as a target for antithrombotic therapy.

Authors:  Charles E Bane; David Gailani
Journal:  Drug Discov Today       Date:  2014-06-02       Impact factor: 7.851

9.  Creating novel activated factor XI inhibitors through fragment based lead generation and structure aided drug design.

Authors:  Ola Fjellström; Sibel Akkaya; Hans-Georg Beisel; Per-Olof Eriksson; Karl Erixon; David Gustafsson; Ulrik Jurva; Daiwu Kang; David Karis; Wolfgang Knecht; Viveca Nerme; Ingemar Nilsson; Thomas Olsson; Alma Redzic; Robert Roth; Jenny Sandmark; Anna Tigerström; Linda Öster
Journal:  PLoS One       Date:  2015-01-28       Impact factor: 3.240

10.  Designing allosteric inhibitors of factor XIa. Lessons from the interactions of sulfated pentagalloylglucopyranosides.

Authors:  Rami A Al-Horani; Umesh R Desai
Journal:  J Med Chem       Date:  2014-05-29       Impact factor: 7.446
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