1. New non peptidic C5a receptor antagonists
- Author
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Tahir N. Majid, Barry Porter, Iain Mcfarlane Mclay, Andrew J. Ratcliffe, Frank Halley, Walsh Roger John Aitchison, Andrew David Morley, Clive McCarthy, Peter M. Lockey, Paul Joseph Cox, T. J. Brown, and Peter Charles Astles
- Subjects
Organic Chemistry ,Clinical Biochemistry ,Antagonist ,Pharmaceutical Science ,Complement C5a ,Pharmacology ,Biochemistry ,Chemical synthesis ,C5a receptor ,In vitro ,Respiratory burst ,chemistry.chemical_compound ,chemistry ,Drug Discovery ,Molecular Medicine ,Molecular Biology ,IC50 ,Lead compound - 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
- 1997
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