Carbazates as potent inhibitors of hormone-sensitive lipase
Carbazates as potent inhibitors of hormone-sensitive lipase
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DOI：
10.1016/j.bmcl.2004.01.038
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发表时间：
2004-04-05
影响因子：
2.7
通讯作者：
Jacobsen, P
中科院分区：
文献类型：
--
作者：
de Jong, JC;Sorensen, LG;Jacobsen, P
脂肪组织脂肪敏感脂肪酶在调节脂肪酸代谢中的核心作用使其成为预防肥胖、前驱糖尿病和糖尿病个体外周胰岛素抵抗的潜在药理学靶点。本文报道了一系列新的肼基甲酸酯的合成。在一系列1，2，3，4-四氢异喹啉和吗啉衍生的肼基甲酸酯中的酚4-位的修饰产生了具有纳摩尔效力的该酶的催化活性的抑制剂。(C)2004爱思唯尔有限公司保留所有权利。
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.