Document Detail

Synthesis and evaluation of a novel indoledione class of long chain fatty acid elongase 6 (ELOVL6) inhibitors.
MedLine Citation:
PMID:  19388647     Owner:  NLM     Status:  MEDLINE    
Novel indoledione derivatives were synthesized and evaluated as long chain fatty acid elongase 6 (ELOVL6) inhibitors. Systematic optimization of an indole class of lead 1 led to the identification of potent ELOVL6 selective inhibitors. Representative inhibitor 37 showed sustained plasma exposure and good liver penetrability in mice. After oral administration, 37 potently inhibited ELOVL6 activity in the liver in mice.
Toshiyuki Takahashi; Tsuyoshi Nagase; Takahide Sasaki; Akira Nagumo; Ken Shimamura; Yasuhisa Miyamoto; Hidefumi Kitazawa; Maki Kanesaka; Ryo Yoshimoto; Katsumi Aragane; Shigeru Tokita; Nagaaki Sato
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Journal of medicinal chemistry     Volume:  52     ISSN:  1520-4804     ISO Abbreviation:  J. Med. Chem.     Publication Date:  2009 May 
Date Detail:
Created Date:  2009-05-22     Completed Date:  2009-07-17     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9716531     Medline TA:  J Med Chem     Country:  United States    
Other Details:
Languages:  eng     Pagination:  3142-5     Citation Subset:  IM    
Tsukuba Research Institute, Merck Research Laboratories, Banyu Pharmaceutical Co., Ltd, Okubo 3, Tsukuba, Ibaraki 300-2611, Japan.
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MeSH Terms
Acetyltransferases / antagonists & inhibitors*
Administration, Oral
Drug Stability
Enzyme Inhibitors / blood,  chemical synthesis*,  pharmacokinetics,  pharmacology*
Indoles / chemical synthesis*,  pharmacology
Liver / metabolism
Structure-Activity Relationship
Reg. No./Substance:
0/Enzyme Inhibitors; 0/Indoles; EC 2.3.1.-/Acetyltransferases; EC 2.3.1.-/fatty acid elongases

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