403986-47-0Relevant academic research and scientific papers
Synthesis and biological activity of L-tyrosine-based PPARγ agonists with reduced molecular weight
Liu, Kevin G.,Lambert, Millard H.,Ayscue, Andrea H.,Henke, Brad R.,Leesnitzer, Lisa M.,Oliver, Jr., William R.,Plunket, Kelli D.,Xu,Sternbach, Daniel D.,Willson, Timothy M.
, p. 3111 - 3113 (2007/10/03)
A series of PPARγ agonists were synthesized from L-tyrosine that incorporated low molecular weight N-substituents. The most potent analogue, pyrrole (4e), demonstrated a Ki of 6.9 nM and an EC50 of 4.7 nM in PPARγ binding and functional assays, respectively. Pyrrole (4e), which is readily synthesized from L-tyrosine methyl ester in four steps, also demonstrated in vivo activity in a rodent model of Type 2 diabetes.
