Pyrrolopyrazinedione-based inhibitors of human hormone-sensitive lipase.
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.
Slee
Deborah H
DH
Ontogen Corporation, 6451 El Camino Real, Carlsbad, California 92009, USA. Debbie.slee@ontogen.com
Bhat
Abhijit S
AS
Nguyen
Truc N
TN
Kish
Mary
M
Lundeen
Katy
K
Newman
Michael J
MJ
McConnell
Stephen J
SJ
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
D004791:Enzyme Inhibitors; D011719:Pyrazines; D002787:Sterol Esterase