Novel, potent and selective chimeric FXa inhibitors featuring hydrophobic P1-ketoamide moieties |
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Authors: | Semple J E Levy O E Minami N K Owens T D Siev D V |
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Institution: | Department of Medicinal Chemistry, Corvas International, Inc., San Diego, CA 92121, USA. ed_semple@corvas.com |
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Abstract: | Judicious combination of P-region sequences of highly potent anticoagulant proteins including NAP5, NAP6, Ecotin, and Antistasin with SAR from small molecule FXa inhibitors led to a series of chimeric inhibitors of formula 1a-j. We report herein the design, synthesis, and biological activity of this novel family of FXa inhibitors that express both high in vitro potency and superb selectivity against related serine proteases. |
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