Synthesis and characterization of 5,6,7,8-tetrahydroquinoline C5a receptor antagonists

Synthesis and structure–activity relationships of a series of substituted 5,6,7,8-tetrahydroquinoline C5a receptor antagonists are reported. A novel series of substituted 2-aryl-5-amino-5,6,7,8-tetrahydroquinoline C5a receptor antagonists is reported. Synthetic routes were developed that allow the substituents on the tetrahydroquinoline core to be efficiently varied, facilitating determination of structure–activity relationships. Members of the series display high binding affinity for the C5a receptor and are potent functional antagonists.