1. ChemInform Abstract: New Non Peptidic C5a Receptor Antagonists
- Author
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Walsh Roger John Aitchison, Tahir N. Majid, Peter Charles Astles, Andrew J. Ratcliffe, Barry Porter, Iain Mcfarlane Mclay, Paul Joseph Cox, Peter M. Lockey, Clive McCarthy, Andrew David Morley, Frank Halley, and T. J. Brown
- Subjects
chemistry.chemical_compound ,Human neutrophil ,Chemistry ,Stereochemistry ,General Medicine ,IC50 ,Lead compound ,C5a receptor ,Respiratory burst ,Functional antagonism - Abstract
A series of phenylguanidines which bind to the C5a receptor has been developed. The lead compound 1 (IC50=30μM), discovered through random screening, has been modified to provide 32 (RPR121154) with submicromolar activity. This compound was shown to further elicit functional antagonism in a human neutrophil C5a stimulated respiratory burst assay.
- Published
- 2010
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