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.
MeSH terms
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Amines / chemistry
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Humans
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Microsomes, Liver / drug effects
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Microsomes, Liver / metabolism
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Molecular Structure
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Quinolines / chemical synthesis*
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Quinolines / chemistry
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Quinolines / pharmacology*
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Receptor, Anaphylatoxin C5a / antagonists & inhibitors*
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Receptor, Anaphylatoxin C5a / metabolism
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Structure-Activity Relationship
Substances
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Amines
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Quinolines
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Receptor, Anaphylatoxin C5a
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5,6,7,8-tetrahydroquinoline