Small, non-peptide C5a receptor antagonists: part 2.
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.
Blagg
Julian
J
Department of Discovery Chemistry, Pfizer Global Research and Development, Ramsgate Road, Sandwich, Kent CT13 9NJ, UK.
Mowbray
Charles
C
Pryde
David
D
Salmon
Gary
G
Fairman
David
D
Schmid
Esther
E
Beaumont
Kevin
K
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
D000577:Amides; D010455:Peptides; D010880:Piperidines; D015936:Complement C5a