申请人:The Scripps Research Institute
公开号:EP2093220A2
公开(公告)日:2009-08-26
Improved competitive inhibitors of fatty acid amide hydrolase (FAAH) employ an alpha-keto heterocyclic pharmacophore and a binding subunit having a pi-unsaturation. The alpha-keto heterocyclic pharmacophore and a binding subunit are attached to one another, preferably by a hydrocarbon chain. The improvement lies in the use of a heterocyclic pharmacophore selected from oxazoles, oxadiazoles, thiazoles, and thiadiazoles that have alkyl or aryl substituents at their 4 and/or 5 positions. The improved competitive inhibitors of FAAH display enhanced activity over conventional competitive inhibitors of FAAH.
改进的脂肪酸酰胺水解酶(FAAH)竞争性抑制剂采用了α-酮杂环药源和具有对不饱和度的结合亚基。α-酮杂环药基和结合亚基彼此连接,最好是通过烃链连接。改进之处在于使用了选自噁唑、噁二唑、噻唑和噻二唑的杂环嗜药体,这些杂环嗜药体的 4 和/或 5 位具有烷基或芳基取代基。与传统的 FAAH 竞争性抑制剂相比,改进的 FAAH 竞争性抑制剂显示出更强的活性。