Abstract
The optimisation of a series of amides for C5a receptor binding and functional activity, and physicochemical properties is described. The initial hit, 1 (IC(50) 1 microM), was discovered during high throughput screening, from which highly potent C5a receptor antagonists (e.g.14, IC(50) 5 nM) were developed.
MeSH terms
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Administration, Oral
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Buffers
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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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Hydrogen-Ion Concentration
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Hydrolysis
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Inhibitory Concentration 50
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Microsomes, Liver / metabolism
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Models, Chemical
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Peptides / chemistry*
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Piperidines / chemistry
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Protein Binding
Substances
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Buffers
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Peptides
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Piperidines
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Complement C5a