Pyrazolone methylamino piperidine derivatives as novel CCR3 antagonists.
The discovery and optimization of a novel class of potent CCR3 antagonists is described. Details of synthesis and SAR are given together with some ADME properties of selected compounds. An optimal balance between activities, physicochemical properties, and in vitro metabolic stability was reached by the proper choice of substituents.
Pégurier
Cécile
C
UCB Pharma SA, R&D, Chemin du Foriest, B-1420 Braine-L'Alleud, Belgium. cecile.pegurier@ucb-group.com
Collart
Philippe
P
Danhaive
Pierre
P
Defays
Sabine
S
Gillard
Michel
M
Gilson
Frédéric
F
Kogej
Thierry
T
Pasau
Patrick
P
Van Houtvin
Nathalie
N
Van Thuyne
Marc
M
van Keulen
BerendJan
B
D006801:Humans; D010880:Piperidines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D054397:Receptors, CCR3; D019707:Receptors, Chemokine / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
C515350:CCR3 protein, human; D010880:Piperidines; D054397:Receptors, CCR3; D019707:Receptors, Chemokine