| Literature DB >> 16464576 |
Christopher Fotsch1, 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.
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.Entities:
Mesh：
Substances：
Year: 2006 PMID： 16464576 DOI： 10.1016/j.bmcl.2006.01.069
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823