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Bioorg Med Chem Lett. 2006 Apr 15;16(8):2071-5. Epub 2006 Feb 7.

A new class of bradykinin 1 receptor antagonists containing the piperidine acetic acid tetralin core.

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Amgen Inc., Department of Chemistry Research and Development, One Amgen Center Drive, Thousand Oaks, CA 91360, USA.


The bradykinin 1 (B1) receptor is upregulated during times of inflammation and is important for maintaining inflamed and chronic pain states. Blocking this receptor has been shown to reverse and/or ameliorate pain and inflammation in animal models. In this report, we describe a new class of B1 receptor antagonists that contain the piperidine acetic acid tetralin core. A structure-activity relationship for these analogs is described in this paper. The most potent compounds from this class have IC50s<20 nM in a B1 receptor functional assay. One of these compounds, 13g, shows modest oral bioavailability in rats.

[Indexed for MEDLINE]

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