克服 hERG 活性，发现一系列 4-氮杂环丁烷-1-芳基环己烷作为 CCR2 拮抗剂。
Overcoming hERG activity in the discovery of a series of 4-azetidinyl-1-aryl-cyclohexanes as CCR2 antagonists.
机构信息
Drug Discovery, Johnson & Johnson Pharmaceutical Research and Development, Welsh & McKean Roads, Box 776, Spring House, PA 19477, United States.
出版信息
Bioorg Med Chem Lett. 2011 Sep 15;21(18):5577-82. doi: 10.1016/j.bmcl.2011.06.080. Epub 2011 Jun 29.
PMID:21783361
Abstract
A series of 4-azetidinyl-1-aryl-cyclohexanes as potent CCR2 antagonists with high selectivity over activity for the hERG potassium channel is discovered through divergent SARs of CCR2 and hERG.
摘要
通过对 CCR2 和 hERG 的发散性 SAR 研究，发现了一系列强效的 CCR2 拮抗剂，它们是 4-氮杂环庚烷-1-芳基环己烷，对 hERG 钾通道具有高选择性和活性。
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