title: The discovery and SAR of cyclopenta[b]furans as inhibitors of CCR2.
abstract: The discovery of a novel series of cyclopenta[b]furans as CCR2 inhibitors is discussed. This series has excellent CCR2 potency and PK characteristics, and good cardiovascular safety.
authors.affiliation: Janssen Research and Development, LLC, 1400 McKean Rd., Spring House, PA 19477, USA. Electronic address: mwinter4@its.jnj.com.
authors.forename: Michael P
authors.initials: MP
authors.lastname: Winters
authors.affiliation: Janssen Research and Development, LLC, 1400 McKean Rd., Spring House, PA 19477, USA.
authors.forename: Christopher A
authors.initials: CA
authors.lastname: Teleha
authors.affiliation: Janssen Research and Development, LLC, 1400 McKean Rd., Spring House, PA 19477, USA.
authors.forename: Fu-An
authors.initials: FA
authors.lastname: Kang
authors.affiliation: Janssen Research and Development, LLC, 1400 McKean Rd., Spring House, PA 19477, USA.
authors.forename: David
authors.initials: D
authors.lastname: McComsey
authors.affiliation: Janssen Research and Development, LLC, 1400 McKean Rd., Spring House, PA 19477, USA.
authors.forename: John C
authors.initials: JC
authors.lastname: O'Neill
authors.affiliation: Janssen Research and Development, LLC, 1400 McKean Rd., Spring House, PA 19477, USA.
authors.forename: Cuifen
authors.initials: C
authors.lastname: Hou
authors.affiliation: Janssen Research and Development, LLC, 1400 McKean Rd., Spring House, PA 19477, USA.
authors.forename: Thomas
authors.initials: T
authors.lastname: Kirchner
authors.affiliation: Janssen Research and Development, LLC, 1400 McKean Rd., Spring House, PA 19477, USA.
authors.forename: Ping
authors.initials: P
authors.lastname: Wang
authors.affiliation: Janssen Research and Development, LLC, 1400 McKean Rd., Spring House, PA 19477, USA.
authors.forename: Dana
authors.initials: D
authors.lastname: Johnson
authors.affiliation: Janssen Research and Development, LLC, 1400 McKean Rd., Spring House, PA 19477, USA.
authors.forename: Zhihua
authors.initials: Z
authors.lastname: Sui
mesh_terms: D002460:Cell Line; D018932:Chemokine CCL2 / Q000276:immunology; D005663:Furans / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D054390:Receptors, CCR2 / Q000037:antagonists & inhibitors* / Q000276:immunology
chemical_list: D018932:Chemokine CCL2; D005663:Furans; D054390:Receptors, CCR2
keywords: CCR2; Cyclopenta[b]furan; MCP-1; Thioglycolate-induced peritoneal leukocyte infiltration model; Type II diabetes