Synthesis and characterization of 5,6,7,8-tetrahydroquinoline C5a receptor antagonists |
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Authors: | Barbay J Kent Gong Yong Buntinx Mieke Li Jian Claes Concha Hornby Pamela J Van Lommen Guy Van Wauwe Jean He Wei |
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Affiliation: | Drug Discovery, Johnson & Johnson PRD, East Coast RED, Spring House, PA 19477-0776, USA. kbarbay@prdus.jnj.com |
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Abstract: | 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. |
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