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
收藏
页码：5639 / 5647
页数：9
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