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.
Denonne
Frédéric
F
UCB Global Chemistry, Chemin du Foriest, R4, 1420 Braine l'Alleud, Belgium. frederic.denonne@ucb-group.com
Binet
Sophie
S
Burton
Maggi
M
Collart
Philippe
P
Defays
Sabine
S
Dipesa
Alan
A
Eckert
Maria
M
Giannaras
Alexander
A
Kumar
Seema
S
Levine
Beth
B
Nicolas
Jean-Marie
JM
Pasau
Patrick
P
Pégurier
Cécile
C
Preda
Dorin
D
Van houtvin
Nathalie
N
Volosov
Andrew
A
Zou
Dong
D
D000588:Amines / Q000737:chemistry*; D000818:Animals; D003167:Complement Activation / Q000187:drug effects*; D008024:Ligands; D008565:Membrane Proteins / Q000378:metabolism*; D051379:Mice; D008807:Mice, Inbred BALB C; D010880:Piperidines / Q000138:chemical synthesis / Q000494:pharmacology*; D011485:Protein Binding; D017346:Protein Serine-Threonine Kinases / Q000378:metabolism; D011951:Receptors, Complement / Q000378:metabolism*; D013329:Structure-Activity Relationship
D000588:Amines; D008024:Ligands; D008565:Membrane Proteins; D010880:Piperidines; D011951:Receptors, Complement; C085567:complement C3a receptor; D017346:Protein Serine-Threonine Kinases