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The synthesis of substituted bipiperidine amide compounds as CCR3 antagonists |
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| Authors: | 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 |
| Affiliation: | Schering Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. pauline.ting@spcorp.com |
| Abstract: | 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. |
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