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.
Basic Information
ID: ALA1158455
Journal: J Med Chem
Title: 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.
Authors: Nagase T, Takahashi T, Sasaki T, Nagumo A, Shimamura K, Miyamoto Y, Kitazawa H, Kanesaka M, Yoshimoto R, Aragane K, Tokita S, Sato N.
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.
CiteXplore: 19522500
DOI: 10.1021/jm900488k
Patent ID: ┄