Synthesis and evaluation of acylguanidine FXa inhibitors |
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| Authors: | O'Connor Stephen P Atwal Karnail Li Chi Liu Eddie C-K Seiler Steven M Shi Mengxiao Shi Yan Stein Philip D Wang Ying |
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| Institution: | Department of Discovery Chemistry, Bristol-Myers Squibb Research and Development, PO Box 5400, Princeton, NJ 08543-5400, USA. steve.oconnor@bms.com |
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| 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 IC(50) of 6 nM. |
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