title: Small, non-peptide C5a receptor antagonists: part 1.
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.
authors.affiliation: Department of Discovery Chemistry, Pfizer Global Research and Development, Ramsgate Road, Sandwich, Kent CT13 9NJ, UK.
authors.forename: Julian
authors.initials: J
authors.lastname: Blagg
authors.forename: Charles
authors.initials: C
authors.lastname: Mowbray
authors.forename: David C
authors.initials: DC
authors.lastname: Pryde
authors.forename: Gary
authors.initials: G
authors.lastname: Salmon
authors.forename: Esther
authors.initials: E
authors.lastname: Schmid
authors.forename: David
authors.initials: D
authors.lastname: Fairman
authors.forename: Kevin
authors.initials: K
authors.lastname: Beaumont
mesh_terms: D000284:Administration, Oral; D002021:Buffers; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D015936:Complement C5a / Q000037:antagonists & inhibitors* / Q000737:chemistry; D015195:Drug Design; D006801:Humans; D006863:Hydrogen-Ion Concentration; D006868:Hydrolysis; D020128:Inhibitory Concentration 50; D008862:Microsomes, Liver / Q000378:metabolism; D008956:Models, Chemical; D010455:Peptides / Q000737:chemistry*; D010880:Piperidines / Q000737:chemistry; D011485:Protein Binding
chemical_list: D002021:Buffers; D010455:Peptides; D010880:Piperidines; D015936:Complement C5a