New non peptidic C5a receptor antagonists

被引:22
作者
Astles, PC
Brown, TJ
Cox, P
Halley, F
Lockey, PM
McCarthy, C
McLay, IM
Majid, TN
Morley, AD
Porter, B
Ratcliffe, AJ
Walsh, RJA
机构
[1] Rhône-Poulenc Rorer, Dagenham Research Centre, Dagenham, Essex, RM10 7XS, Rainham Road South
关键词
HUMAN ANAPHYLATOXIN C5A; BINDING; IDENTIFICATION; NITRILES; SEGMENT;
D O I
10.1016/S0960-894X(97)00124-8
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of phenylguanidines which bind to the C5a receptor has been developed. The lead compound 1 (IC50=30 mu M), 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. (C) 1997 Elsevier Science Ltd.
引用
收藏
页码:907 / 912
页数:6
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