Chiral 1, 3, 4-oxadiazol-2-ones as highly selective FAAH inhibitors

…, JR Savinainen, D Navia-Paldanius…

文献索引：Patel, Jayendra Z.; Parkkari, Teija; Laitinen, Tuomo; Kaczor, Agnieszka A.; Saario, Susanna M.; Savinainen, Juha R.; Navia-Paldanius, Dina; Cipriano, Mariateresa; Leppaenen, Jukka; Koshevoy, Igor O.; Poso, Antti; Fowler, Christopher J.; Laitinen, Jarmo T.; Nevalainen, Tapio Journal of Medicinal Chemistry, 2013 , vol. 56, # 21 p. 8484 - 8496

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被引用次数: 18

摘要

In the present study, identification of chiral 1, 3, 4-oxadiazol-2-ones as potent and selective FAAH inhibitors has been described. The separated enantiomers showed clear differences in the potency and selectivity toward both FAAH and MAGL. Additionally, the importance of the chirality on the inhibitory activity and selectivity was proven by the simplification approach by removing a methyl group at the 3-position of the 1, 3, 4-oxadiazol-2-one ring. ...