title: Substituted dipiperidine alcohols as potent CCR2 antagonists.
abstract: The synthesis and biological evaluation of a series of substituted dipiperidine alcohols are described. Structure-activity relationship studies led to the discovery of potent CCR2 antagonists displaying IC(50) values in the nanomolar or subnanomolar range. The cinnamoyl compounds had higher binding affinities than the corresponding urea analogs.
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: James
authors.initials: J
authors.lastname: Brackley
authors.forename: Monica
authors.initials: M
authors.lastname: Singer
authors.forename: Michele
authors.initials: M
authors.lastname: Matheis
authors.forename: Druie
authors.initials: D
authors.lastname: Cavender
authors.forename: Michael
authors.initials: M
authors.lastname: Wachter
mesh_terms: D000438:Alcohols / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001665:Binding Sites; D004353:Drug Evaluation, Preclinical; D006801:Humans; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D010880:Piperidines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D054390:Receptors, CCR2 / Q000037:antagonists & inhibitors*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D000438:Alcohols; D010880:Piperidines; D054390:Receptors, CCR2