904962-32-9Relevant articles and documents
Synthesis and structure-activity relationships of N-{3-[2-(4-alkoxyphenoxy) thiazol-5-yl]-1-methylprop-2-ynyl}carboxy derivatives as selective acetyl-CoA carboxylase 2 inhibitors
Gu, Yu Gui,Weitzberg, Moshe,Clark, Richard F.,Xu, Xiangdong,Li, Qun,Zhang, Tianyuan,Hansen, T. Matthew,Liu, Gang,Xin, Zhili,Wang, Xiaojun,Wang, Rongqi,McNally, Teresa,Camp, Heidi,Beutel, Bruce A.,Sham, Hing L.
, p. 3770 - 3773 (2007/10/03)
A structurally novel acetyl-CoA carboxylase (ACC) inhibitor is identified from high-throughput screening. A preliminary structure-activity relationship study led to the discovery of potent dual ACC1/ACC2 and ACC2 selective inhibitors against human recombinant ACC1 and ACC2. Selective ACC2 inhibitors exhibited IC50 1000-fold selectivity against ACC1. (S)-Enantiomer 9p exhibited high ACC2 activity and lowered muscle malonyl-CoA dose-dependently in acute rodent studies, whereas (R)-enantiomer 9o was weak and had no effect on the malonyl-CoA level.