New non peptidic C5a receptor antagonists

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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.

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 (RPR120033) with submicromolar activity. This compound was shown to further elicit functional antagonism in a human neutrophil C5a stimulated respiratory burst assay

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