Abstract
Starting from 2, several highly potent C5a receptor antagonists were synthesised through alpha-amide substitution. Attempts to increase the polarity of these compounds through the introduction of basic centres or incorporation into weakly basic heterocycles is described.
MeSH terms
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Administration, Oral
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Amides / chemistry*
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Binding Sites
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Chemistry, Pharmaceutical / methods*
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Complement C5a / antagonists & inhibitors*
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Complement C5a / chemistry
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Drug Design
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Humans
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Hydrolysis
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Inflammation
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Inhibitory Concentration 50
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Models, Chemical
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Molecular Structure
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Peptides / chemistry*
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Piperidines / chemistry
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Protein Binding
Substances
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Amides
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Peptides
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Piperidines
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Complement C5a