Pyrrolopyrazinedione-based inhibitors of human hormone-sensitive lipase

被引：32

作者：

Slee, DH ^{[1
]}

Bhat, AS ^{[1
]}

Nguyen, TN ^{[1
]}

Kish, M ^{[1
]}

Lundeen, K ^{[1
]}

Newman, MJ ^{[1
]}

McConnell, SJ ^{[1
]}

机构：

[1] Ontogen Corp, Carlsbad, CA 92009 USA

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2003年 / 46卷 / 07期

关键词：

D O I：

10.1021/jm020460y

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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 C-14-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.

引用

页码：1120 / 1122

页数：3

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