3-Arylamino-2H-1,2,4-benzothiadiazin-5-ol 1,1-dioxides as novel and selective CXCR2 antagonists.
A series of 3-arylamino-2H-1,2,4-benzothiadiazin-5-ol 1,1-dioxides were prepared and shown to be novel and selective antagonists of the CXCR2 receptor. Synthesis, structure and activity relationships, selectivity, and some developability properties are described.
Wang
Yonghui
Y
Discovery Medicinal Chemistry, Molecular Discovery Research, GlaxoSmithKline, 1250 South Collegeville Road, Collegeville, PA 19426, USA. yonghui.2.wang@gsk.com
Busch-Petersen
Jakob
J
Wang
Feng
F
Ma
Lanping
L
Fu
Wei
W
Kerns
Jeffrey K
JK
Jin
Jian
J
Palovich
Michael R
MR
Shen
Jing-Kang
JK
Burman
Miriam
M
Foley
James J
JJ
Schmidt
Dulcie B
DB
Hunsberger
Gerald E
GE
Sarau
Henry M
HM
Widdowson
Katherine L
KL
D001581:Benzothiadiazines / Q000737:chemistry / Q000494:pharmacology*; D023063:Receptors, Interleukin-8B / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
D001581:Benzothiadiazines; D023063:Receptors, Interleukin-8B