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

Bioorg Med Chem Lett

Drug Discovery, Johnson & Johnson PRD, East Coast RED, Spring House, PA 19477-0776, USA.

Published: April 2008

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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http://dx.doi.org/10.1016/j.bmcl.2008.03.049DOI Listing

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