title: Identification of a sulfonamide series of CCR2 antagonists.
abstract: A series of sulfonamide CCR2 antagonists was identified by high-throughput screening. Management of molecular weight and physical properties, in particular moderation of lipophilicity and study of pK(a), yielded highly potent CCR2 antagonists exhibiting good pharmacokinetic properties and improved potency in the presence of human plasma.
authors.affiliation: GlaxoSmithKline Medicines Research Centre, Stevenage, UK. Simon.2.Peace@gsk.com
authors.forename: Simon
authors.initials: S
authors.lastname: Peace
authors.forename: Joanne
authors.initials: J
authors.lastname: Philp
authors.forename: Carl
authors.initials: C
authors.lastname: Brooks
authors.forename: Val
authors.initials: V
authors.lastname: Piercy
authors.forename: Kitty
authors.initials: K
authors.lastname: Moores
authors.forename: Chris
authors.initials: C
authors.lastname: Smethurst
authors.forename: Steve
authors.initials: S
authors.lastname: Watson
authors.forename: Simon
authors.initials: S
authors.lastname: Gaines
authors.forename: Mara
authors.initials: M
authors.lastname: Zippoli
authors.forename: Claudette
authors.initials: C
authors.lastname: Mookherjee
authors.forename: Robert
authors.initials: R
authors.lastname: Ife
mesh_terms: D000818:Animals; D004305:Dose-Response Relationship, Drug; D057166:High-Throughput Screening Assays; D006801:Humans; D051379:Mice; D015394:Molecular Structure; D054389:Receptors, CCR1 / Q000037:antagonists & inhibitors; D054390:Receptors, CCR2 / Q000037:antagonists & inhibitors*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D054389:Receptors, CCR1; D054390:Receptors, CCR2; D013449:Sulfonamides