title: Design and synthesis of novel small molecule CCR2 antagonists: evaluation of 4-aminopiperidine derivatives.
abstract: A novel N-(2-oxo-2-(piperidin-4-ylamino)ethyl)-3-(trifluoromethyl)benzamide series of human CCR2 chemokine receptor antagonists was identified. With a pharmacophore model based on known CCR2 antagonists a new core scaffold was designed, analogues of it synthesized and structure–affinity relationship studies derived yielding a new high affinity CCR2 antagonist N-(2-((1-(4-(3-methoxyphenyl)cyclohexyl)piperidin-4-yl)amino)-2-oxoethyl)-3-(trifluoromethyl)benzamide.
authors.forename: M
authors.initials: M
authors.lastname: Vilums
authors.forename: A J M
authors.initials: AJ
authors.lastname: Zweemer
authors.forename: S
authors.initials: S
authors.lastname: Dekkers
authors.forename: Y
authors.initials: Y
authors.lastname: Askar
authors.forename: H
authors.initials: H
authors.lastname: de Vries
authors.forename: J
authors.initials: J
authors.lastname: Saunders
authors.forename: D
authors.initials: D
authors.lastname: Stamos
authors.forename: J
authors.initials: J
authors.lastname: Brussee
authors.forename: L H
authors.initials: LH
authors.lastname: Heitman
authors.forename: A P
authors.initials: AP
authors.lastname: IJzerman
mesh_terms: D018925:Chemokines; D006801:Humans; D015394:Molecular Structure; D010880:Piperidines / Q000737:chemistry*; D054390:Receptors, CCR2 / Q000037:antagonists & inhibitors* / Q000737:chemistry; D013329:Structure-Activity Relationship
chemical_list: C481395:4-aminopiperidine; D018925:Chemokines; D010880:Piperidines; D054390:Receptors, CCR2