Carbazates as potent inhibitors of hormone-sensitive lipase.

Bioorg Med Chem Lett

Novo Nordisk A/S, Medicinal Chemistry, Novo Nordisk Park, 2760 Maaloev, Denmark.

Published: April 2004

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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http://dx.doi.org/10.1016/j.bmcl.2004.01.038DOI Listing

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