Synthesis and evaluation of a novel 2-azabicyclo[2.2.2]octane class of long chain fatty acid elongase 6 (ELOVL6) inhibitors

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...

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Veröffentlicht in:	Bioorganic & medicinal chemistry 2009-08, Vol.17 (15), p.5639-5647
Hauptverfasser:	Sasaki, Takahide, Nagase, Tsuyoshi, Takahashi, Toshiyuki, Nagumo, Akira, Shimamura, Ken, Miyamoto, Yasuhisa, Kitazawa, Hidefumi, Kanesaka, Maki, Yoshimoto, Ryo, Aragane, Katsumi, Tokita, Shigeru, Sato, Nagaaki
Format:	Artikel
Sprache:	eng
Schlagworte:	2-Azabicyclo[2.2.2]octane Acetyltransferases - antagonists & inhibitors Acetyltransferases - metabolism Animals Anti-diabetic agent Azabicyclo Compounds - chemical synthesis Azabicyclo Compounds - chemistry Azabicyclo Compounds - pharmacokinetics Azabicyclo Compounds - pharmacology Biological and medical sciences Fatty Acids - metabolism General and cellular metabolism. Vitamins Humans Lipogenesis Liver - enzymology Long chain fatty acid elongase 6 inhibitor Male Medical sciences Mice Mice, Inbred C57BL Octanes - chemical synthesis Octanes - chemistry Octanes - pharmacokinetics Octanes - pharmacology Pharmacology. Drug treatments Structure-Activity Relationship
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Zusammenfassung:	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.
ISSN:	0968-0896 1464-3391
DOI:	10.1016/j.bmc.2009.06.042