Small, non-peptide C5a receptor antagonists: part 1

  • Bioorg Med Chem Lett. 2008 Oct 15;18(20):5601-4. doi: 10.1016/j.bmcl.2008.08.106.
Julian Blagg  1 ,  Charles Mowbray ,  David C Pryde ,  Gary Salmon ,  Esther Schmid ,  David Fairman ,  Kevin Beaumont
Affiliations
  • 1. Department of Discovery Chemistry, Pfizer Global Research and Development, Ramsgate Road, Sandwich, Kent CT13 9NJ, UK.
PMID: 18809326 DOI: 10.1016/j.bmcl.2008.08.106
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.

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