The complement C3a receptor and its native ligand, C3a protein, have been linked to a number of inflammatory diseases including asthma, arthritis, diabetes, obesity and allergy. Incorporating 5-membered heterocycles into peptides and small molecules has led to the discovery of discrete pharmacophores for agonist and antagonist activity. Structure-activity relationship studies have been conducted on heterocyclic ligands leading to significant advances in achieving high potency and drug-like properties. The syntheses, structures and activities of some potent small molecule ligands that bind to the human C3a receptor will be reported.

Recent advances in potent heterocyclic modulators of complement C3a receptor

251st National Meeting (2016)

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