New non peptidic C5a receptor antagonists

…, F Halley, PM Lockey, C McCarthy, IM McLay…

文献索引：Astles, Peter C.; Brown, Thomas J.; Cox, Paul; Halley, Frank; Lockey, Peter M.; McCarthy, Clive; McLay, Iain M.; Majid, Tahir N.; Morley, Andrew D.; Porter, Barry; Ratcliffe, Andrew J.; Walsh, Roger J.A. Bioorganic and Medicinal Chemistry Letters, 1997 , vol. 7, # 7 p. 907 - 912

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被引用次数: 21

摘要

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.