具有螺环二胺核心的杂芳基脲类作为脂肪酸酰胺水解酶抑制剂
Heteroarylureas with spirocyclic diamine cores as inhibitors of fatty acid amide hydrolase.
作者信息
Keith John M, Jones William M, Pierce Joan M, Seierstad Mark, Palmer James A, Webb Michael, Karbarz Mark J, Scott Brian P, Wilson Sandy J, Luo Lin, Wennerholm Michelle L, Chang Leon, Brown Sean M, Rizzolio Michele, Rynberg Raymond, Chaplan Sandra R, Breitenbucher J Guy
机构信息
Janssen Research and Development, L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA.
Janssen Research and Development, L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA.
出版信息
Bioorg Med Chem Lett. 2014 Feb 1;24(3):737-41. doi: 10.1016/j.bmcl.2013.12.113. Epub 2014 Jan 6.
A series of mechanism based heteroaryl urea fatty acid amide hydrolase (FAAH) inhibitors with spirocyclic diamine cores is described. A potent member of this class, (37), was found to inhibit FAAH centrally, elevate the brain levels of three fatty acid ethanolamides [FAAs: anandamide (AEA), oleoyl ethanolamide (OEA) and palmitoyl ethanolamide (PEA)], and was moderately efficacious in a rat model of neuropathic pain.
描述了一系列具有螺环二胺核心的基于机制的杂芳基脲脂肪酸酰胺水解酶（FAAH）抑制剂。该类中的一个强效成员（37）被发现可在中枢抑制FAAH，提高三种脂肪酸乙醇酰胺[FAA：花生四烯乙醇胺（AEA）、油酰乙醇胺（OEA）和棕榈酰乙醇胺（PEA）]的脑内水平，并且在神经性疼痛大鼠模型中具有中等疗效。
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