Bioorganic and Medicinal Chemistry Letters p. 2071 - 2075 (2006)
Update date:2022-08-11
Topics:
Fotsch, Christopher
Biddlecome, Gloria
Biswas, Kaustav
Chen, Jian Jeff
D'Amico, Derin C.
Groneberg, Robert D.
Han, Nianhe Bruce
Hsieh, Feng-Yin
Kamassah, Augustus
Kumar, Gondi
Lester-Zeiner, Dianna
Liu, Qingyian
Mareska, David A.
Riahi, Babak Bobby
Wang, Yueh-Ju Judy
Yang, Kevin
Zhan, James
Zhu, Joe
Johnson, Eileen
Ng, Gordon
Askew, Benny C.
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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