Premium
Screening of Various Hormone‐Sensitive Lipase Inhibitors as Endocannabinoid‐Hydrolyzing Enzyme Inhibitors
Author(s) -
Minkkilä Anna,
Savinainen Juha R.,
Käsnänen Heikki,
Xhaard Henri,
Nevalainen Tapio,
Laitinen Jarmo T.,
Poso Antti,
Leppänen Jukka,
Saario Susanna M.
Publication year - 2009
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.200900137
Subject(s) - monoacylglycerol lipase , fatty acid amide hydrolase , lipase , hormone sensitive lipase , endocannabinoid system , enzyme , biochemistry , chemistry , monoglyceride , fatty acid , cannabinoid receptor , antagonist , receptor
Various hormone‐sensitive lipase (HSL) inhibitors, such as oxadiazolones, 2 H ‐isoxazol‐5‐ones and carbamoyltriazoles, were evaluated for their fatty acid amide hydrolase (FAAH) and monoglyceride lipase (MGL) inhibitory potencies. All compounds inhibited both enzymes with IC 50 values varying from the nanomolar to low micromolar range. The compounds may serve as lead structures in the development of novel and potentially selective FAAH and MGL inhibitors.