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Camphor sulfonamide derivatives as novel,potent and selective CXCR3 antagonists
Authors: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
Institution:1. Center of Excellence for Drug Discovery, GlaxoSmithKline, 1250 South Collegeville Road, Collegeville, PA 19426, USA;2. Molecular Discovery Research, GlaxoSmithKline, 1250 South Collegeville Road, Collegeville, PA 19426, USA;3. Center of Excellence for Drug Discovery, GlaxoSmithKline, 709 Swedeland Road, King of Prussia, PA 19406, USA
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.
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