Camphor sulfonamide derivatives as novel, potent and selective CXCR3 antagonists

Yonghui Wang; Jakob Busch-Petersen; Feng Wang; Terence J Kiesow; Todd L Graybill; Jian Jin; Zheng Yang; James J Foley; Gerald E Hunsberger; Dulcie B Schmidt; Henry M Sarau; Elizabeth A Capper-Spudich; Zining Wu; Laura S Fisher; Michael S McQueney; Ralph A Rivero; Katherine L Widdowson

doi:10.1016/j.bmcl.2008.11.008

Camphor sulfonamide derivatives as novel, potent and selective CXCR3 antagonists

Bioorg Med Chem Lett. 2009 Jan 1;19(1):114-8. doi: 10.1016/j.bmcl.2008.11.008. Epub 2008 Nov 6.

Authors

Yonghui Wang¹, Jakob Busch-Petersen, Feng Wang, Terence J Kiesow, Todd L Graybill, Jian Jin, Zheng Yang, James J Foley, Gerald E Hunsberger, Dulcie B Schmidt, Henry M Sarau, Elizabeth A Capper-Spudich, Zining Wu, Laura S Fisher, Michael S McQueney, Ralph A Rivero, Katherine L Widdowson

Affiliation

¹ Center of Excellence for Drug Discovery, GlaxoSmithKline, 1250 South Collegeville Road, Collegeville, PA 19426, USA. [email protected]

PMID: 19014886
DOI: 10.1016/j.bmcl.2008.11.008

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.

MeSH terms

Camphor / analogs & derivatives*
Camphor / chemical synthesis
Camphor / pharmacology
Humans
Piperazines
Receptors, CXCR3 / antagonists & inhibitors*
Structure-Activity Relationship
Sulfonamides / chemical synthesis*
Sulfonamides / pharmacology

Substances

CXCR3 protein, human
Piperazines
Receptors, CXCR3
Sulfonamides
Camphor