Discovery of new C3aR ligands. Part 1: Arginine derivatives

The synthesis and in vitro binding of several new arginine-containing C3aR ligands are reported. DMPK properties and functional activities of selected compounds have been evaluated. One compound is shown to be active in an in vivo model of airway inflammation after aerosol administration.

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2007-06, Vol.17 (12), p.3258-3261
Main Authors: Denonne, Frédéric, Binet, Sophie, Burton, Maggi, Collart, Philippe, Dipesa, Alan, Ganguly, Tanmoy, Giannaras, Alexander, Kumar, Seema, Lewis, Timothy, Maounis, Florence, Nicolas, Jean-Marie, Mansley, Tamsin, Pasau, Patrick, Preda, Dorin, Stebbins, Karin, Volosov, Alexander, Zou, Dong
Format: Article
Language:English
Subjects:
Aerosols - administration & dosage
Animals
Arginine
Arginine - analogs & derivatives
Arginine - chemical synthesis
Arginine - pharmacology
Biological and medical sciences
C3a
Complement Activation - drug effects
Inflammation
Inflammation - chemically induced
Inflammation - pathology
Ligands
Medical sciences
Membrane Proteins - metabolism
Mice
Mice, Inbred BALB C
Models, Biological
Pharmacology. Drug treatments
Protein Binding
Protein-Serine-Threonine Kinases - metabolism
Receptors, Complement - metabolism
Respiratory Mucosa - pathology
Respiratory system
Structure-Activity Relationship
Time Factors
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Description
Summary:The synthesis and in vitro binding of several new arginine-containing C3aR ligands are reported. DMPK properties and functional activities of selected compounds have been evaluated. One compound is shown to be active in an in vivo model of airway inflammation after aerosol administration.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2007.04.022