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

Bioorganic & Medicinal Chemistry Letters（2009）

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摘要

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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关键词

Camphor sulfonamides,N-arylpiperazine,CXCR3 receptor antagonists,Chemokine,GPCRs,Inflammation

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