Synthesis and evaluation of a novel 2-azabicyclo[2.2.2]octane class of long chain fatty acid elongase 6 (ELOVL6) inhibitors

被引：3

作者：

Sasaki, Takahide ^{[1
]}

Nagase, Tsuyoshi ^{[1
]}

Takahashi, Toshiyuki ^{[1
]}

Nagumo, Akira ^{[1
]}

Shimamura, Ken ^{[1
]}

Miyamoto, Yasuhisa ^{[1
]}

Kitazawa, Hidefumi ^{[1
]}

Kanesaka, Maki ^{[1
]}

Yoshimoto, Ryo ^{[1
]}

Aragane, Katsumi ^{[1
]}

Tokita, Shigeru ^{[1
]}

Sato, Nagaaki ^{[1
,2
]}

机构：

[1] Banyu Pharmaceut Co Ltd, Merck Res Labs, Tsukuba Res Inst, Tsukuba, Ibaraki 3002611, Japan

[2] Taisho Pharmaceut Co Ltd, Taisho Res Labs, Kita Ku, Saitama 3319530, Japan

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2009年 / 17卷 / 15期

关键词：

Long chain fatty acid elongase 6 inhibitor; 2-Azabicyclo[2.2.2]octane; Anti-diabetic agent; Lipogenesis; ACYL-COA ELONGASE; ADIPOSE-TISSUE; GENE FAMILY; IDENTIFICATION; METABOLISM; CLONING;

D O I：

10.1016/j.bmc.2009.06.042

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A series of novel 2-azabicyclo[2.2.2]octane derivatives was synthesized and evaluated as long chain fatty acid elongase 6 (ELOVL6) inhibitors. Screening of our corporate chemical collections against ELOVL6 resulted in the identification of lead 1. Exploratory chemistry efforts were applied to lead 1 to identify the orally available, potent, and selective ELOVL6 inhibitor 28a. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：5639 / 5647

页数：9

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