title: Discovery of new C3aR ligands. Part 1: arginine derivatives.
abstract: 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.
authors.affiliation: UCB Global Chemistry, Chemin du Foriest R4, 1420 Braine l'Alleud, Belgium. frederic.denonne@ucb-group.com
authors.forename: Frédéric
authors.initials: F
authors.lastname: Denonne
authors.forename: Sophie
authors.initials: S
authors.lastname: Binet
authors.forename: Maggi
authors.initials: M
authors.lastname: Burton
authors.forename: Philippe
authors.initials: P
authors.lastname: Collart
authors.forename: Alan
authors.initials: A
authors.lastname: Dipesa
authors.forename: Tanmoy
authors.initials: T
authors.lastname: Ganguly
authors.forename: Alexander
authors.initials: A
authors.lastname: Giannaras
authors.forename: Seema
authors.initials: S
authors.lastname: Kumar
authors.forename: Timothy
authors.initials: T
authors.lastname: Lewis
authors.forename: Florence
authors.initials: F
authors.lastname: Maounis
authors.forename: Jean-Marie
authors.initials: JM
authors.lastname: Nicolas
authors.forename: Tamsin
authors.initials: T
authors.lastname: Mansley
authors.forename: Patrick
authors.initials: P
authors.lastname: Pasau
authors.forename: Dorin
authors.initials: D
authors.lastname: Preda
authors.forename: Karin
authors.initials: K
authors.lastname: Stebbins
authors.forename: Alexander
authors.initials: A
authors.lastname: Volosov
authors.forename: Dong
authors.initials: D
authors.lastname: Zou
mesh_terms: D000336:Aerosols / Q000008:administration & dosage; D000818:Animals; D001120:Arginine / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000494:pharmacology*; D003167:Complement Activation / Q000187:drug effects*; D007249:Inflammation / Q000139:chemically induced / Q000473:pathology; D008024:Ligands; D008565:Membrane Proteins / Q000378:metabolism*; D051379:Mice; D008807:Mice, Inbred BALB C; D008954:Models, Biological; D011485:Protein Binding; D017346:Protein Serine-Threonine Kinases / Q000378:metabolism; D011951:Receptors, Complement / Q000378:metabolism*; D020545:Respiratory Mucosa / Q000473:pathology; D013329:Structure-Activity Relationship; D013997:Time Factors
chemical_list: D000336:Aerosols; D008024:Ligands; D008565:Membrane Proteins; D011951:Receptors, Complement; C085567:complement C3a receptor; D001120:Arginine; D017346:Protein Serine-Threonine Kinases