Title of article
Synthesis and evaluation of acylguanidine FXa inhibitors
Author/Authors
Stephen P. O’Connor، نويسنده , , Karnail Atwal، نويسنده , , Chi Li، نويسنده , , Eddie C. -K. Liu، نويسنده , , Steven M. Seiler، نويسنده , , Mengxiao Shi، نويسنده , , Yan Shi، نويسنده , , Philip D. Stein، نويسنده , , Ying Wang، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
4
From page
4696
To page
4699
Abstract
A series of acylguanidine derivatives were prepared and investigated as inhibitors of Factor Xa (FXa). These compounds were made by guanidine acylation with carboxylic acids using carbonyl diimidazole (CDI) as the coupling reagent. Conditions for the rapid synthesis and purification of these compounds are described along with their ability to inhibit FXa. The best FXa inhibitor is 1 with a FXa IC50 of 6 nM.
Keywords
coagulation , factor Xa , serine protease
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
799862
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