The synthesis of substituted bipiperidine amide compounds as CCR3 antagonists

…, Y Huang, J Jakway, J Kelly, Z Liu, S McCombie…

文献索引：Ting, Pauline C.; Lee, Joe F.; Wu, Jie; Umland, Shelby P.; Aslanian, Robert; Cao, Jianhua; Dong, Youhao; Garlisi, Charles G.; Gilbert, Eric J.; Huang, Ying; Jakway, James; Kelly, Joseph; Liu, Zhidan; McCombie, Stuart; Shah, Himanshu; Tian, Fang; Wan, Yuntao; Shih, Neng-Yang Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 5 p. 1375 - 1378

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被引用次数: 39

摘要

Bipiperidine amide 1 has been identified as a CC chemokine receptor 3 (CCR3) antagonist. Optimization of its structure–activity relationship has resulted in the identification of cis (R, R)- 4-[(3, 4-dichlorophenyl) methyl]-3-hydroxymethyl-1′(6-quinolinylcarbonyl)-1, 4′- bipiperidine 14n, which exhibits potent receptor affinity and inhibition of both calcium flux and eosinophil chemotaxis.