Synthesis and structure–activity relationships of heteroaryl substituted-3, 4-diamino-3-cyclobut-3-ene-1, 2-dione CXCR2/CXCR1 receptor antagonists

…, D Rindgen, R Bond, R Mayer-Ezel, J Jakway…

文献索引：Yu, Younong; Dwyer, Michael P.; Chao, Jianping; Aki, Cynthia; Chao, Jianhua; Purakkattle, Biju; Rindgen, Diane; Bond, Richard; Mayer-Ezel, Rosemary; Jakway, James; Qiu, Hongchen; Hipkin, R. William; Fossetta, James; Gonsiorek, Waldemar; Bian, Hong; Fan, Xuedong; Terminelli, Carol; Fine, Jay; Lundell, Daniel; Merritt, J. Robert; He, Zhenmin; Lai, Gaifa; Wu, Minglang; Taveras, Arthur Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 4 p. 1318 - 1322

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被引用次数: 15

摘要

Comprehensive SAR studies were undertaken in the 3, 4-diaminocyclobut-3-ene-1, 2-dione class of CXCR2/CXCR1 receptor antagonists to explore the role of the heterocycle on chemokine receptor binding affinities, functional activity, as well as oral exposure in rat. The nature of the heterocycle as well as the requisite substitution pattern around the heterocycle was shown to have a dramatic effect on the overall biological profile of this class of ...