title: Synthesis and structure-activity relationship of 7-azaindole piperidine derivatives as CCR2 antagonists.
abstract: The synthesis and structure-activity relationship of a series of 7-azaindole piperidine derivatives are described. SAR studies led to the discovery of the potent CCR2 antagonists displaying IC(50) values in the nanomolar range. The representative compound 15 showed reasonable P450 and pharmacokinetics profile.
authors.affiliation: Drug Discovery, Johnson & Johnson Pharmaceutical Research and Development, L.L.C., 8 Clarke Drive, Cranbury, NJ 08512, USA. mxia@prdus.jnj.com
authors.forename: Mingde
authors.initials: M
authors.lastname: Xia
authors.forename: Cuifen
authors.initials: C
authors.lastname: Hou
authors.forename: Duane
authors.initials: D
authors.lastname: DeMong
authors.forename: Scott
authors.initials: S
authors.lastname: Pollack
authors.forename: Meng
authors.initials: M
authors.lastname: Pan
authors.forename: Monica
authors.initials: M
authors.lastname: Singer
authors.forename: Michele
authors.initials: M
authors.lastname: Matheis
authors.forename: William
authors.initials: W
authors.lastname: Murray
authors.forename: Druie
authors.initials: D
authors.lastname: Cavender
authors.forename: Michael
authors.initials: M
authors.lastname: Wachter
mesh_terms: D000438:Alcohols / Q000737:chemistry; D001665:Binding Sites; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D018932:Chemokine CCL2 / Q000737:chemistry*; D015195:Drug Design; D006801:Humans; D007211:Indoles / Q000737:chemistry*; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D010880:Piperidines / Q000737:chemistry*; D054390:Receptors, CCR2 / Q000037:antagonists & inhibitors* / Q000737:chemistry*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D000438:Alcohols; C111835:CCL2 protein, human; C515334:CCR2 protein, human; D018932:Chemokine CCL2; D007211:Indoles; D010880:Piperidines; D054390:Receptors, CCR2; C032727:piperidine