Small, non-peptide C5a receptor antagonists: Part 2

▪ Starting from 2, several highly potent C5a receptor antagonists were synthesised through α-amide substitution. Attempts to increase the polarity of these compounds through the introduction of basic centres or incorporation into weakly basic heterocycles is described.

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Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry 2008-10, Vol.18 (20), p.5605-5608
Hauptverfasser:	Blagg, Julian, Mowbray, Charles, Pryde, David, Salmon, Gary, Fairman, David, Schmid, Esther, Beaumont, Kevin
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Oral Amides - chemistry Antagonists Binding Sites Biological and medical sciences Bones, joints and connective tissue. Antiinflammatory agents C5a Receptor Chemistry, Pharmaceutical - methods Complement Complement C5a - antagonists & inhibitors Complement C5a - chemistry Drug Design Humans Hydrolysis Inflammation Inhibitory Concentration 50 Medical sciences Models, Chemical Molecular Structure Peptides - chemistry Pharmacology. Drug treatments Piperidines - chemistry Protein Binding
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Beschreibung
Zusammenfassung:	▪ Starting from 2, several highly potent C5a receptor antagonists were synthesised through α-amide substitution. Attempts to increase the polarity of these compounds through the introduction of basic centres or incorporation into weakly basic heterocycles is described.
ISSN:	0960-894X 0968-0896 1464-3405 1464-3391
DOI:	10.1016/j.bmcl.2008.08.101