Author/Authors :
Takahide Sasaki، نويسنده , , Tsuyoshi Nagase، نويسنده , , Toshiyuki Takahashi، نويسنده , , Akira Nagumo، نويسنده , , Ken Shimamura، نويسنده , , Yasuhisa Miyamoto، نويسنده , , Hidefumi Kitazawa، نويسنده , , Maki Kanesaka، نويسنده , , Ryo Yoshimoto، نويسنده , , Katsumi Aragane، نويسنده , , Shigeru Tokita، نويسنده , , Nagaaki Sato، نويسنده ,
Abstract :
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.