title: Small, non-peptide C5a receptor antagonists: part 2.
abstract: Starting from 2, several highly potent C5a receptor antagonists were synthesised through alpha-amide substitution. Attempts to increase the polarity of these compounds through the introduction of basic centres or incorporation into weakly basic heterocycles is described.
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
authors.initials: D
authors.lastname: Pryde
authors.forename: Gary
authors.initials: G
authors.lastname: Salmon
authors.forename: David
authors.initials: D
authors.lastname: Fairman
authors.forename: Esther
authors.initials: E
authors.lastname: Schmid
authors.forename: Kevin
authors.initials: K
authors.lastname: Beaumont
mesh_terms: D000284:Administration, Oral; D000577:Amides / Q000737:chemistry*; D001665:Binding Sites; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D015936:Complement C5a / Q000037:antagonists & inhibitors* / Q000737:chemistry; D015195:Drug Design; D006801:Humans; D006868:Hydrolysis; D007249:Inflammation; D020128:Inhibitory Concentration 50; D008956:Models, Chemical; D015394:Molecular Structure; D010455:Peptides / Q000737:chemistry*; D010880:Piperidines / Q000737:chemistry; D011485:Protein Binding
chemical_list: D000577:Amides; D010455:Peptides; D010880:Piperidines; D015936:Complement C5a