title: Conformationally restricted indolopiperidine derivatives as potent CCR2B receptor antagonists.
abstract: The preparation and biological evaluation of a series of indolopiperidine CCR2B receptor antagonists possessing a conformationally restricted C-5 linker chain in combination with a restricted piperidine ring are described. Compared to the parent compound 1, analogue 8 shows a dramatic improvement in selectivity against a range of 5-HT and dopaminergic receptors.
authors.affiliation: Department of Discovery Chemistry, GlaxoSmithKline Pharmaceuticals, New Frontiers Science Park, Third Avenue, Harlow, CM19 5AD, Essex, UK. jason_withering@sbphrd.com
authors.forename: J
authors.initials: J
authors.lastname: Witherington
authors.forename: V
authors.initials: V
authors.lastname: Bordas
authors.forename: D G
authors.initials: DG
authors.lastname: Cooper
authors.forename: I T
authors.initials: IT
authors.lastname: Forbes
authors.forename: A D
authors.initials: AD
authors.lastname: Gribble
authors.forename: R J
authors.initials: RJ
authors.lastname: Ife
authors.forename: T
authors.initials: T
authors.lastname: Berkhout
authors.forename: J
authors.initials: J
authors.lastname: Gohil
authors.forename: P H
authors.initials: PH
authors.lastname: Groot
mesh_terms: D018492:Dopamine Antagonists / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D007211:Indoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D008968:Molecular Conformation; D010880:Piperidines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D054390:Receptors, CCR2; D019707:Receptors, Chemokine / Q000037:antagonists & inhibitors* / Q000378:metabolism; D012702:Serotonin Antagonists / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D018492:Dopamine Antagonists; D007211:Indoles; D010880:Piperidines; D054390:Receptors, CCR2; D019707:Receptors, Chemokine; D012702:Serotonin Antagonists; C435666:indolopiperidine