Synthesis and characterization of 5,6,7,8-tetrahydroquinoline C5a receptor antagonists.
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.
Barbay
J Kent
JK
Drug Discovery, Johnson & Johnson PRD, East Coast RED, Spring House, PA 19477-0776, USA. kbarbay@prdus.jnj.com
Gong
Yong
Y
Buntinx
Mieke
M
Li
Jian
J
Claes
Concha
C
Hornby
Pamela J
PJ
Van Lommen
Guy
G
Van Wauwe
Jean
J
He
Wei
W
D000588:Amines / Q000737:chemistry; D006801:Humans; D008862:Microsomes, Liver / Q000187:drug effects / Q000378:metabolism; D015394:Molecular Structure; D011804:Quinolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D044087:Receptor, Anaphylatoxin C5a / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship
D000588:Amines; D011804:Quinolines; D044087:Receptor, Anaphylatoxin C5a; C528846:5,6,7,8-tetrahydroquinoline