title: Carbazates as potent inhibitors of hormone-sensitive lipase.
abstract: The central role of adipose tissue hormone-sensitive lipase in regulating fatty acid metabolism makes it a potential pharmacological target for the prevention of peripheral insulin resistance in obese, prediabetic and diabetic individuals. The synthesis of a new series of carbazates is presented. Modification of the phenolic 4-position in a series of 1,2,3,4-tetrahydroisoquinoline and morpholine derived carbazates, yielded inhibitors of the catalytic activity of this enzyme with nanomolar potency.
authors.affiliation: Novo Nordisk A/S, Medicinal Chemistry, Novo Nordisk Park, 2760 Maaloev, Denmark.
authors.forename: Johannes C
authors.initials: JC
authors.lastname: de Jong
authors.forename: Lotte G
authors.initials: LG
authors.lastname: Sørensen
authors.forename: Hans
authors.initials: H
authors.lastname: Tornqvist
authors.forename: Poul
authors.initials: P
authors.lastname: Jacobsen
mesh_terms: D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology; D006834:Hydrazines / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology; D002787:Sterol Esterase / Q000037:antagonists & inhibitors* / Q000378:metabolism
chemical_list: D004791:Enzyme Inhibitors; D006834:Hydrazines; C010877:carbazic acid; D002787:Sterol Esterase