2. Academic Validation
  3. Carbazates as potent inhibitors of hormone-sensitive lipase

Carbazates as potent inhibitors of hormone-sensitive lipase

  • Bioorg Med Chem Lett. 2004 Apr 5;14(7):1741-4. doi: 10.1016/j.bmcl.2004.01.038.
Johannes C de Jong 1,  Lotte G Sørensen,  Hans Tornqvist,  Poul Jacobsen
Affiliations

Affiliation

  • 1 Novo Nordisk A/S, Medicinal Chemistry, Novo Nordisk Park, 2760 Maaloev, Denmark.
PMID: 15026062 DOI: 10.1016/j.bmcl.2004.01.038
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.

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