Synthesis and evaluation of a novel indoledione class of long chain fatty acid elongase 6 (ELOVL6) inhibitors.
Basic Information
ID: ALA1138496
Journal: J Med Chem
Title: Synthesis and evaluation of a novel indoledione class of long chain fatty acid elongase 6 (ELOVL6) inhibitors.
Authors: Takahashi T, Nagase T, Sasaki T, Nagumo A, Shimamura K, Miyamoto Y, Kitazawa H, Kanesaka M, Yoshimoto R, Aragane K, Tokita S, Sato N.
Abstract: 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.
CiteXplore: 19388647
DOI: 10.1021/jm900391x
Patent ID: ┄