Carbazates as potent inhibitors of hormone-sensitive lipase

被引：30

作者：

de Jong, JC

Sorensen, LG

Tornqvist, H

Jacobsen, P

机构：

[1] Novo Nordisk AS, Med Chem, DK-2760 Malov, Denmark

[2] Novo Nordisk AS, Assay & Cell Technol, DK-2880 Bagsvaerd, Denmark

[3] Novo Nordisk AS, Diabet Biol, DK-2760 Malov, Denmark

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 07期

关键词：

hormone-sensitive lipase; inhibition; carbazates;

D O I：

10.1016/j.bmcl.2004.01.038

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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. (C) 2004 Elsevier Ltd. All rights reserved.

引用

收藏

页码：1741 / 1744

页数：4

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