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

  • J Med Chem. 2009 Jul 23;52(14):4111-4. doi: 10.1021/jm900488k.
Tsuyoshi Nagase  1 ,  Toshiyuki Takahashi ,  Takahide Sasaki ,  Akira Nagumo ,  Ken Shimamura ,  Yasuhisa Miyamoto ,  Hidefumi Kitazawa ,  Maki Kanesaka ,  Ryo Yoshimoto ,  Katsumi Aragane ,  Shigeru Tokita ,  Nagaaki Sato
Affiliations
  • 1. Tsukuba Research Institute, Merck Research Laboratories, Banyu Pharmaceutical Co, Ltd, Tsukuba, Ibaraki 300-2611, Japan. [email protected]
PMID: 19522500 DOI: 10.1021/jm900488k
Abstract

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.

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