Synthesis and Biological Evaluation of a Novel 3-Sulfonyl-8-azabicyclo[3.2.1]octane Class of Long Chain Fatty Acid Elongase 6 (ELOVL6) Inhibitors
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- 作者：Tsuyoshi Nagase ; Toshiyuki Takahashi ; Takahide Sasaki ; Akira Nagumo ; Ken Shimamura ; Yasuhisa Miyamoto ; Hidefumi Kitazawa ; Maki Kanesaka ; Ryo Yoshimoto ; Katsumi Aragane ; Shigeru Tokita ; Nagaaki Sato
- 刊名：Journal of Medicinal Chemistry
- 出版年：2009
- 出版时间：July 23, 2009
- 年：2009
- 卷：52
- 期：14
- 页码：4111-4114
- 全文大小：690K
- 年卷期：v.52,no.14(July 23, 2009)
- ISSN：1520-4804
文摘
Long chain fatty acid elongase 6 (ELOVL6) catalyzes the elongation of long chain fatty acyl-CoAs and is a potential target for the treatment of metabolic disorders. The ultrahigh throughput screen of our corporate chemical collections resulted in the identification of a novel 3-sulfonyl-8-azabicyclo[3.2.1]octane class of ELOVL6 inhibitor 1a. Optimization of lead 1a led to the identification of the potent, selective, and orally available ELOVL6 inhibitor 1w.