Novel benzo-fused lactam scaffolds as factor Xa inhibitors. |
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Authors: | S Y Tamura E A Goldman P W Bergum J E Semple |
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Affiliation: | Corvas International, Inc., Department of Medicinal Chemistry, San Diego, California 92121, USA. |
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Abstract: | Rigid benzolactam P3-P2 dipeptide mimics were designed and prepared as potential inhibitors of blood coagulation factor Xa. Methoxy substitution of the tetrahydrobenzazepinone scaffold led to potent and selective inhibitors. The synthesis and biological activities of these derivatives are reported herein. |
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