NEW NON PEPTIDIC C5A RECEPTOR ANTAGONISTS

Authors
ASTLES PC BROWN TJ COX P HALLEY F LOCKEY PM MCCARTHY C MCLAY IM MAJID TN MORLEY AD PORTER B RATCLIFFE AJ WALSH RJA
Citation
Pc. Astles et al., NEW NON PEPTIDIC C5A RECEPTOR ANTAGONISTS, Bioorganic & medicinal chemistry letters, 7(7), 1997, pp. 907-912
Citations number
13
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
7
Issue
7
Year of publication
1997
Pages
907 - 912
Database
ISI
SICI code
0960-894X(1997)7:7<907:NNPCRA>2.0.ZU;2-N
Abstract
A series of phenylguanidines which bind to the C5a receptor has been d eveloped. The lead compound 1 (IC50=30 mu M), discovered through rando m screening, has been modified to provide 32 (RPR121154) with submicro molar activity. This compound was shown to further elicit functional a ntagonism in a human neutrophil C5a stimulated respiratory burst assay . (C) 1997 Elsevier Science Ltd.