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Bioorg Med Chem Lett. 2008 Aug 15;18(16):4477-81. doi: 10.1016/j.bmcl.2008.07.055. Epub 2008 Jul 17.

Discovery of dihydroquinoxalinone acetamides containing bicyclic amines as potent Bradykinin B1 receptor antagonists.

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Chemistry Research and Development, Amgen Inc., One Amgen Center Drive, MS-B29-4-1-B, Thousand Oaks, CA 91320, USA.


Replacement of the core beta-amino acid in our previously reported piperidine acetic acid and beta-phenylalanine-based Bradykinin B1 antagonists by dihydroquinoxalinone acetic acid increases the in vitro potency and metabolic stability. The most potent compounds from this series have IC(50)s<0.2 nM in a human B1 receptor functional assay. A molecular modeling study of the binding modes of key compounds, based on a B1 homology model, explains the structure-activity relationship (SAR) for these analogs.

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