501029-92-1Relevant academic research and scientific papers
Antidiabetic agents
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, (2008/06/13)
The present invention provides compounds of Formula (I): wherein A, X, Q, Y, B, D, Z, and E have any of the values defined in the specification, and pharmaceutically acceptable salt thereof, that are useful as antidiabetic agents. Also disclosed are pharmaceutical compositions comprising one or more compounds of Formula I, processes for preparing compounds of Formula I, and intermediates useful for preparing compounds of Formula I.
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.
