title: 3-Arylamino-2H-1,2,4-benzothiadiazin-5-ol 1,1-dioxides as novel and selective CXCR2 antagonists.
abstract: 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.
authors.affiliation: Discovery Medicinal Chemistry, Molecular Discovery Research, 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: Lanping
authors.initials: L
authors.lastname: Ma
authors.forename: Wei
authors.initials: W
authors.lastname: Fu
authors.forename: Jeffrey K
authors.initials: JK
authors.lastname: Kerns
authors.forename: Jian
authors.initials: J
authors.lastname: Jin
authors.forename: Michael R
authors.initials: MR
authors.lastname: Palovich
authors.forename: Jing-Kang
authors.initials: JK
authors.lastname: Shen
authors.forename: Miriam
authors.initials: M
authors.lastname: Burman
authors.forename: James J
authors.initials: JJ
authors.lastname: Foley
authors.forename: Dulcie B
authors.initials: DB
authors.lastname: Schmidt
authors.forename: Gerald E
authors.initials: GE
authors.lastname: Hunsberger
authors.forename: Henry M
authors.initials: HM
authors.lastname: Sarau
authors.forename: Katherine L
authors.initials: KL
authors.lastname: Widdowson
mesh_terms: D001581:Benzothiadiazines / Q000737:chemistry / Q000494:pharmacology*; D023063:Receptors, Interleukin-8B / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: D001581:Benzothiadiazines; D023063:Receptors, Interleukin-8B