Christopher Fotsch,
Gloria Biddlecome,
Kaustav Biswas,
Jian Jeff Chen,
Derin C D'Amico,
Robert D Groneberg,
Nianhe Bruce Han,
Feng-Yin Hsieh,
Augustus Kamassah,
Gondi Kumar, [......],
Qingyian Liu,
David A Mareska,
Babak Bobby Riahi,
Yueh-Ju Judy Wang,
Kevin Yang,
James Zhan, Joe Zhu,
Eileen Johnson,
Gordon Ng,
Benny C Askew
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ABSTRACT: 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.
Bioorganic & Medicinal Chemistry Letters 04/2006; 16(8):2071-5. · 2.55 Impact Factor
