| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1374454 | Bioorganic & Medicinal Chemistry Letters | 2009 | 5 Pages |
Abstract
A novel series of small molecule C5a antagonists is reported. In particular, in vitro metabolic studies and solution based combinatorial synthesis are demonstrated as useful tools for the rapid identification of antagonists with low in vitro clearance. Members of this series specifically inhibited the binding of 125I-labeled C5a to human recombinant C5a receptor (C5aR). In functional cell assays these compounds displayed surmountable antagonism against C5a and did not demonstrate any detectable agonist activity.
Graphical abstractA novel series of small molecule C5a antagonists is reported.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Hitesh J. Sanganee, Andrew Baxter, Simon Barber, Alastair J.H. Brown, Denise Grice, Fraser Hunt, Sarah King, David Laughton, Garry Pairaudeau, Bob Thong, Richard Weaver, John Unitt,