title: Pyrrolopyrazinedione-based inhibitors of human hormone-sensitive lipase.
abstract: The regulation of lipid metabolism and it's effect on glucose control and diabetes has received intense interest. Hormone-sensitive lipase (HSL) is a vital enzyme in lipid metabolism. A series of novel pyrrolopyrazinediones has been discovered that demonstrate submicromolar activity both in the enzyme assay and in a (14)C-emulsion assay employing cholesteryl oleate as a substrate as a secondary measure of HSL activity. These compounds represent novel inhibitors of the human HSL enzyme.
authors.affiliation: Ontogen Corporation, 6451 El Camino Real, Carlsbad, California 92009, USA. Debbie.slee@ontogen.com
authors.forename: Deborah H
authors.initials: DH
authors.lastname: Slee
authors.forename: Abhijit S
authors.initials: AS
authors.lastname: Bhat
authors.forename: Truc N
authors.initials: TN
authors.lastname: Nguyen
authors.forename: Mary
authors.initials: M
authors.lastname: Kish
authors.forename: Katy
authors.initials: K
authors.lastname: Lundeen
authors.forename: Michael J
authors.initials: MJ
authors.lastname: Newman
authors.forename: Stephen J
authors.initials: SJ
authors.lastname: McConnell
mesh_terms: D000818:Animals; D002460:Cell Line; D016208:Databases, Factual; D004353:Drug Evaluation, Preclinical; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D007313:Insecta / Q000166:cytology; D011719:Pyrazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002787:Sterol Esterase / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: D004791:Enzyme Inhibitors; D011719:Pyrazines; D002787:Sterol Esterase