Document Detail


Synthesis and evaluation of a novel 2-azabicyclo[2.2.2]octane class of long chain fatty acid elongase 6 (ELOVL6) inhibitors.
MedLine Citation:
PMID:  19596583     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
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.
Authors:
Takahide Sasaki; Tsuyoshi Nagase; Toshiyuki Takahashi; 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     Date:  2009-06-26
Journal Detail:
Title:  Bioorganic & medicinal chemistry     Volume:  17     ISSN:  1464-3391     ISO Abbreviation:  Bioorg. Med. Chem.     Publication Date:  2009 Aug 
Date Detail:
Created Date:  2009-07-21     Completed Date:  2009-10-13     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  9413298     Medline TA:  Bioorg Med Chem     Country:  England    
Other Details:
Languages:  eng     Pagination:  5639-47     Citation Subset:  IM    
Affiliation:
Tsukuba Research Institute, Merck Research Laboratories, Banyu Pharmaceutical Co., Ltd, Okubo 3, Tsukuba, Ibaraki 300-2611, Japan.
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MeSH Terms
Descriptor/Qualifier:
Acetyltransferases / antagonists & inhibitors*,  metabolism*
Animals
Azabicyclo Compounds / chemical synthesis,  chemistry*,  pharmacokinetics,  pharmacology*
Fatty Acids / metabolism
Humans
Liver / enzymology
Male
Mice
Mice, Inbred C57BL
Octanes / chemical synthesis,  chemistry*,  pharmacokinetics,  pharmacology*
Structure-Activity Relationship
Chemical
Reg. No./Substance:
0/Azabicyclo Compounds; 0/Fatty Acids; 0/Octanes; 111-65-9/octane; EC 2.3.1.-/Acetyltransferases; EC 2.3.1.-/fatty acid elongases

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