采用四氢-1,3-恶嗪-2-酮间隔基的基于尿素的CCR3拮抗剂。
Urea based CCR3 antagonists employing a tetrahydro-1,3-oxazin-2-one spacer.
作者信息
Dhar T G Murali, Yang Guchen, Davies Paul, Malley Mary F, Gougoutas Jack Z, Wu Dauh-Rurng, Barrish Joel C, Carter Percy H
机构信息
Bristol-Myers Squibb Company, Research and Development, Princeton, NJ 08543-4000, USA.
出版信息
Bioorg Med Chem Lett. 2009 Jan 1;19(1):96-9. doi: 10.1016/j.bmcl.2008.11.002. Epub 2008 Nov 6.
Conformational restriction of open chain analogs with a more polar tetrahydro-1,3-oxazin-2-one spacer led to the identification of potent urea-based CCR3 antagonists that exhibited excellent selectivity over binding to CYP2D6. The in vitro binding and eosinophil shape change data are presented. Compound 19b exhibited similar selectivity and potency to our development candidate BMS-639623.
具有更具极性的四氢-1,3-恶嗪-2-酮间隔基的开链类似物的构象限制导致了强效脲基CCR3拮抗剂的鉴定，这些拮抗剂在与CYP2D6结合方面表现出优异的选择性。给出了体外结合和嗜酸性粒细胞形态变化数据。化合物19b表现出与我们的研发候选药物BMS-639623相似的选择性和效力。
Zotero 插件