1.
Bioorg Med Chem Lett
; 19(4): 1143-7, 2009 Feb 15.
Artículo
en Inglés
| MEDLINE
| ID: mdl-19171482
RESUMEN
A novel series of small molecule C5a antagonists is reported. In particular, in vitro metabolic studies and solution based combinatorial synthesis are demonstrated as useful tools for the rapid identification of antagonists with low in vitro clearance. Members of this series specifically inhibited the binding of (125)I-labeled C5a to human recombinant C5a receptor (C5aR). In functional cell assays these compounds displayed surmountable antagonism against C5a and did not demonstrate any detectable agonist activity.