- A new class of bradykinin 1 receptor antagonists containing the piperidine acetic acid tetralin core.
A new class of bradykinin 1 receptor antagonists containing the piperidine acetic acid tetralin core.
Bioorganic & medicinal chemistry letters (2006-02-09)
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, Dianna Lester-Zeiner, 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
PMID16464576
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.
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