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Bioorg Med Chem Lett. 2008 Oct 15;18(20):5601-4. doi: 10.1016/j.bmcl.2008.08.106. Epub 2008 Aug 31.

Small, non-peptide C5a receptor antagonists: part 1.

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1
Department of Discovery Chemistry, Pfizer Global Research and Development, Ramsgate Road, Sandwich, Kent CT13 9NJ, UK.

Abstract

The optimisation of a series of amides for C5a receptor binding and functional activity, and physicochemical properties is described. The initial hit, 1 (IC(50) 1 microM), was discovered during high throughput screening, from which highly potent C5a receptor antagonists (e.g.14, IC(50) 5 nM) were developed.

PMID:
18809326
DOI:
10.1016/j.bmcl.2008.08.106
[Indexed for MEDLINE]
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