Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1376174 | Bioorganic & Medicinal Chemistry Letters | 2008 | 4 Pages |
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.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Stephen P. O’Connor, Karnail Atwal, Chi Li, Eddie C.-K. Liu, Steven M. Seiler, Mengxiao Shi, Yan Shi, Philip D. Stein, Ying Wang,