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Bioorg Med Chem Lett. 2009 Feb 15;19(4):1143-7. doi: 10.1016/j.bmcl.2008.12.104. Epub 2008 Dec 31.

Discovery of small molecule human C5a receptor antagonists.

Author information

1
AstraZeneca R&D Charnwood, Medicinal Chemistry, Bakewell Road, Loughborough, LE11 5RH, UK. Hitesh.sanganee@astrazeneca.com

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 (125)I-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.

PMID:
19171482
DOI:
10.1016/j.bmcl.2008.12.104
[Indexed for MEDLINE]

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