脂肪酸酰胺水解酶抑制剂。3：具有体内活性的四取代氮杂环丁烷脲。
Fatty acid amide hydrolase inhibitors. 3: tetra-substituted azetidine ureas with in vivo activity.
机构信息
Vernalis (R&D) Ltd, Granta Park, Cambridge CB21 6GB, UK.
出版信息
Bioorg Med Chem Lett. 2012 Jan 15;22(2):901-6. doi: 10.1016/j.bmcl.2011.12.032. Epub 2011 Dec 13.
PMID:22209458
Abstract
We describe here our attempts to optimise the human fatty acid amide hydrolase (FAAH) inhibition and physicochemical properties of our previously reported tetrasubstituted azetidine urea FAAH inhibitor, VER-156084. We describe the SAR of a series of analogues and conclude with the demonstration of in vivo dose-dependant FAAH inhibition in an anandamide-loading study in rats.
摘要
我们在此描述了优化先前报道的四取代氮杂环丁烷脲 FAAH 抑制剂 VER-156084 的人类脂肪酸酰胺水解酶 (FAAH) 抑制作用和理化性质的尝试。我们描述了一系列类似物的 SAR，并在大鼠中进行的大麻素加载研究中证明了体内剂量依赖性 FAAH 抑制作用。
Zotero 插件