Novel pyrrolidine heterocycles as CCR1 antagonists

…, MJ Ohlmeyer, E Quadros, P Wines, J Postelnek…

文献索引：Merritt, J. Robert; James, Ray; Paradkar, Vidyadhar M.; Zhang, Chongwu; Liu, Ruiyan; Liu, Jinqi; Jacob, Biji; Chiriac, Camelia; Ohlmeyer, Michael J.; Quadros, Elizabeth; Wines, Pamela; Postelnek, Jennifer; Hicks, Catherine M.; Chen, Weiqing; Kimble, Earl F.; O'Brien, Linda; White, Nicole; Desai, Hema; Appell, Kenneth C.; Webb, Maria L. Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 18 p. 5477 - 5479

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被引用次数: 9

摘要

A novel series of pyrrolidine heterocycles was prepared and found to show potent inhibitory activity of CCR1 binding and CCL3 mediated chemotaxis of a CCR1-expressing cell line. A potent, optimized triazole lead from this series was found to have acceptable pharmacokinetics and microsomal stability in rat and is suitable for further optimization and development.