title: Camphor sulfonamide derivatives as novel, potent and selective CXCR3 antagonists.
abstract: A series of N-arylpiperazine camphor sulfonamides was discovered as novel CXCR3 antagonists. The synthesis, structure-activity relationships, and optimization of the initial hit that resulted in the identification of potent and selective CXCR3 antagonists are described.
authors.affiliation: Center of Excellence for Drug Discovery, GlaxoSmithKline, 1250 South Collegeville Road, Collegeville, PA 19426, USA. yonghui.2.wang@gsk.com
authors.forename: Yonghui
authors.initials: Y
authors.lastname: Wang
authors.forename: Jakob
authors.initials: J
authors.lastname: Busch-Petersen
authors.forename: Feng
authors.initials: F
authors.lastname: Wang
authors.forename: Terence J
authors.initials: TJ
authors.lastname: Kiesow
authors.forename: Todd L
authors.initials: TL
authors.lastname: Graybill
authors.forename: Jian
authors.initials: J
authors.lastname: Jin
authors.forename: Zheng
authors.initials: Z
authors.lastname: Yang
authors.forename: James J
authors.initials: JJ
authors.lastname: Foley
authors.forename: Gerald E
authors.initials: GE
authors.lastname: Hunsberger
authors.forename: Dulcie B
authors.initials: DB
authors.lastname: Schmidt
authors.forename: Henry M
authors.initials: HM
authors.lastname: Sarau
authors.forename: Elizabeth A
authors.initials: EA
authors.lastname: Capper-Spudich
authors.forename: Zining
authors.initials: Z
authors.lastname: Wu
authors.forename: Laura S
authors.initials: LS
authors.lastname: Fisher
authors.forename: Michael S
authors.initials: MS
authors.lastname: McQueney
authors.forename: Ralph A
authors.initials: RA
authors.lastname: Rivero
authors.forename: Katherine L
authors.initials: KL
authors.lastname: Widdowson
mesh_terms: D002164:Camphor / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D006801:Humans; D010879:Piperazines; D054367:Receptors, CXCR3 / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: C515187:CXCR3 protein, human; D010879:Piperazines; D054367:Receptors, CXCR3; D013449:Sulfonamides; D002164:Camphor