title: Pyrazolone methylamino piperidine derivatives as novel CCR3 antagonists.
abstract: 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.
authors.affiliation: UCB Pharma SA, R&D, Chemin du Foriest, B-1420 Braine-L'Alleud, Belgium. cecile.pegurier@ucb-group.com
authors.forename: Cécile
authors.initials: C
authors.lastname: Pégurier
authors.forename: Philippe
authors.initials: P
authors.lastname: Collart
authors.forename: Pierre
authors.initials: P
authors.lastname: Danhaive
authors.forename: Sabine
authors.initials: S
authors.lastname: Defays
authors.forename: Michel
authors.initials: M
authors.lastname: Gillard
authors.forename: Frédéric
authors.initials: F
authors.lastname: Gilson
authors.forename: Thierry
authors.initials: T
authors.lastname: Kogej
authors.forename: Patrick
authors.initials: P
authors.lastname: Pasau
authors.forename: Nathalie
authors.initials: N
authors.lastname: Van Houtvin
authors.forename: Marc
authors.initials: M
authors.lastname: Van Thuyne
authors.forename: BerendJan
authors.initials: B
authors.lastname: van Keulen
mesh_terms: D006801:Humans; D010880:Piperidines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D054397:Receptors, CCR3; D019707:Receptors, Chemokine / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: C515350:CCR3 protein, human; D010880:Piperidines; D054397:Receptors, CCR3; D019707:Receptors, Chemokine