title: Potent heteroarylpiperidine and carboxyphenylpiperidine 1-alkyl-cyclopentane carboxamide CCR2 antagonists.
abstract: This report describes replacement of the 4-(4-fluorophenyl)piperidine moiety in our CCR2 antagonists with 4-heteroaryl piperidine and 4-(carboxyphenyl)-piperidine subunits. Some of the resulting analogs retained potency in our CCR2 binding assay and had improved selectivity versus the I(Kr) channel; poor selectivity against I(Kr) had been a liability of earlier analogs in this series.
authors.affiliation: Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, 126 East Lincoln Avenue, Rahway, NJ 07065, USA. alexander_pasternak@merck.com
authors.forename: Alexander
authors.initials: A
authors.lastname: Pasternak
authors.forename: Stephen D
authors.initials: SD
authors.lastname: Goble
authors.forename: Pasquale P
authors.initials: PP
authors.lastname: Vicario
authors.forename: Jerry
authors.initials: J
authors.lastname: Di Salvo
authors.forename: Julia M
authors.initials: JM
authors.lastname: Ayala
authors.forename: Mary
authors.initials: M
authors.lastname: Struthers
authors.forename: Julie A
authors.initials: JA
authors.lastname: DeMartino
authors.forename: Sander G
authors.initials: SG
authors.lastname: Mills
authors.forename: Lihu
authors.initials: L
authors.lastname: Yang
mesh_terms: D000818:Animals; D006801:Humans; D015394:Molecular Structure; D010880:Piperidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D026902:Potassium Channel Blockers / Q000494:pharmacology; D051381:Rats; D054390:Receptors, CCR2 / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: D010880:Piperidines; D026902:Potassium Channel Blockers; D054390:Receptors, CCR2