Bioorganic and Medicinal Chemistry Letters p. 5601 - 5604 (2008)
Update date:2022-09-26
Topics: Therapeutic applications Challenges Mechanism of Action Advantages
Blagg, Julian
Mowbray, Charles
Pryde, David C.
Salmon, Gary
Schmid, Esther
Fairman, David
Beaumont, Kevin
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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