Camphor sulfonamide derivatives as novel, potent and selective CXCR3 antagonists.
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.
Wang
Yonghui
Y
Center of Excellence for Drug Discovery, GlaxoSmithKline, 1250 South Collegeville Road, Collegeville, PA 19426, USA. yonghui.2.wang@gsk.com
Busch-Petersen
Jakob
J
Wang
Feng
F
Kiesow
Terence J
TJ
Graybill
Todd L
TL
Jin
Jian
J
Yang
Zheng
Z
Foley
James J
JJ
Hunsberger
Gerald E
GE
Schmidt
Dulcie B
DB
Sarau
Henry M
HM
Capper-Spudich
Elizabeth A
EA
Wu
Zining
Z
Fisher
Laura S
LS
McQueney
Michael S
MS
Rivero
Ralph A
RA
Widdowson
Katherine L
KL
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
C515187:CXCR3 protein, human; D010879:Piperazines; D054367:Receptors, CXCR3; D013449:Sulfonamides; D002164:Camphor