Small, non-peptide C5a receptor antagonists: Part 1

The optimisation of a series of amides for C5a receptor binding and functional activity, and physicochemical properties is described. The initial hit, 1 (IC50 1 μM), was discovered during high throughput screening, from which highly potent C5a receptor antagonists (e.g.14, IC50 5 nM) were developed.

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