(4-Piperidinyl)-piperazine: A new platform for acetyl-CoA carboxylase inhibitors

被引：20

作者：

Chonan, Tomomichi ^{[1
]}

Oi, Takahiro ^{[1
]}

Yamamoto, Daisuke ^{[2
]}

Yashiro, Miyoko ^{[3
]}

Wakasugi, Daisuke ^{[1
]}

Tanaka, Hiroaki ^{[1
]}

Ohoka-Sugita, Ayumi ^{[2
]}

Io, Fusayo ^{[2
]}

Koretsune, Hiroko ^{[2
]}

Hiratate, Akira ^{[1
]}

机构：

[1] Taisho Pharmaceut Co Ltd, Med Chem Labs, Kita Ku, Saitama 3319530, Japan

[2] Taisho Pharmaceut Co Ltd, Mol Funct & Pharmacol Labs, Kita Ku, Saitama 3319530, Japan

[3] Taisho Pharmaceut Co Ltd, Res Comp Syst, Kita Ku, Saitama 3319530, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 23期

关键词：

Acetyl-CoA carboxylase; Inhibitor; (4-Piperidinyl)-piperazine; FATTY-ACID OXIDATION; COENZYME;

D O I：

10.1016/j.bmcl.2009.10.012

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Acetyl-CoA carboxylases (ACCs), the rate limiting enzymes in de novo lipid synthesis, play important roles in modulating energy metabolism. The inhibition of ACC has demonstrated promising therapeutic potential for treating obesity and type 2 diabetes mellitus in transgenic mice and preclinical animal models. We describe herein the synthesis and structure-activity relationships of a series of disubstituted (4-piperidinyl)-piperazine derivatives as a new platform for ACC1/2 non-selective inhibitors. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：6645 / 6648

页数：4

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