Title of article
Synthesis and in vitro biological evaluation of aryl boronic acids as potential inhibitors of factor Xia
Author/Authors
Tsvetelina I. Lazarova، نويسنده , , Lei Jin، نويسنده , , Michael Rynkiewicz، نويسنده , , Joan C. Gorga، نويسنده , , Frank Bibbins، نويسنده , , Harold V. Meyers، نويسنده , , Robert Babine، نويسنده , , James Strickler، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2006
Pages
6
From page
5022
To page
5027
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.
Keywords
Trypsin , Factor XIa , factor Xa , Aryl boronic acids , thrombin
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2006
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
797322
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