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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1997年 / 7卷 / 07期

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

页码：907 / 912

页数：6

共 13 条

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BROWN HC, 1981, SYNTHESIS-STUTTGART, P605

[2]

CAPDEVIELLE P, 1989, SYNTHESIS-STUTTGART, P451

[3]

DOSEOP K, 1995, ACS NAT M CHIC IL AU

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