title: Design, synthesis, and structure-activity relationship of novel CCR2 antagonists.
abstract: A series of novel 1-aminocyclopentyl-3-carboxyamides incorporating substituted tetrahydropyran moieties have been synthesized and subsequently evaluated for their antagonistic activity against the human CCR2 receptor. Among them analog 59 was found to posses potent antagonistic activity.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA.
authors.forename: Shankaran
authors.initials: S
authors.lastname: Kothandaraman
authors.forename: Karla L
authors.initials: KL
authors.lastname: Donnely
authors.forename: Gabor
authors.initials: G
authors.lastname: Butora
authors.forename: Richard
authors.initials: R
authors.lastname: Jiao
authors.forename: Alexander
authors.initials: A
authors.lastname: Pasternak
authors.forename: Gregori J
authors.initials: GJ
authors.lastname: Morriello
authors.forename: Stephen D
authors.initials: SD
authors.lastname: Goble
authors.forename: Changyou
authors.initials: C
authors.lastname: Zhou
authors.forename: Sander G
authors.initials: SG
authors.lastname: Mills
authors.forename: Malcolm
authors.initials: M
authors.lastname: Maccoss
authors.forename: Pasquale P
authors.initials: PP
authors.lastname: Vicario
authors.forename: Julia M
authors.initials: JM
authors.lastname: Ayala
authors.forename: Julie A
authors.initials: JA
authors.lastname: Demartino
authors.forename: Mary
authors.initials: M
authors.lastname: Struthers
authors.forename: Margaret A
authors.initials: MA
authors.lastname: Cascieri
authors.forename: Lihu
authors.initials: L
authors.lastname: Yang
mesh_terms: D000284:Administration, Oral; D000818:Animals; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D002633:Chemotaxis; D004285:Dogs; D015195:Drug Design; D006801:Humans; D020128:Inhibitory Concentration 50; D008253:Macaca mulatta; D008956:Models, Chemical; D015394:Molecular Structure; D051381:Rats; D017207:Rats, Sprague-Dawley; D054390:Receptors, CCR2 / Q000037:antagonists & inhibitors* / Q000737:chemistry*; D013329:Structure-Activity Relationship
chemical_list: D054390:Receptors, CCR2