Discovery of new C3aR ligands. Part 2: Amino-piperidine derivatives

The synthesis and structure–activity relationships against the C3a receptor of a series of substituted aminopiperidine derivatives are reported. DMPK properties and functional activities of selected compounds are described. The compounds obtained are the first non-arginine ligands of C3aR.

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2007-06, Vol.17 (12), p.3262-3265
Hauptverfasser:	Denonne, Frédéric, Binet, Sophie, Burton, Maggi, Collart, Philippe, Defays, Sabine, Dipesa, Alan, Eckert, Maria, Giannaras, Alexander, Kumar, Seema, Levine, Beth, Nicolas, Jean-Marie, Pasau, Patrick, Pégurier, Cécile, Preda, Dorin, Van houtvin, Nathalie, Volosov, Andrew, Zou, Dong
Format:	Artikel
Sprache:	eng
Schlagworte:	Agonist Amines - chemistry Animals Biological and medical sciences C3a Complement Activation - drug effects Inflammation Ligands Medical sciences Membrane Proteins - metabolism Mice Mice, Inbred BALB C Pharmacology. Drug treatments Piperidines - chemical synthesis Piperidines - pharmacology Protein Binding Protein-Serine-Threonine Kinases - metabolism Receptors, Complement - metabolism Respiratory system SAR Structure-Activity Relationship
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Beschreibung
Zusammenfassung:	The synthesis and structure–activity relationships against the C3a receptor of a series of substituted aminopiperidine derivatives are reported. DMPK properties and functional activities of selected compounds are described. The compounds obtained are the first non-arginine ligands of C3aR.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2007.04.023