Synthesis and biological activity of L-tyrosine-based PPARgamma agonists with reduced molecular weight.
Article Details
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Liu KG, Lambert MH, Ayscue AH, Henke BR, Leesnitzer LM, Oliver WR Jr, Plunket KD, Xu HE, Sternbach DD, Willson TM
Synthesis and biological activity of L-tyrosine-based PPARgamma agonists with reduced molecular weight.
Bioorg Med Chem Lett. 2001 Dec 17;11(24):3111-3.
- PubMed ID
- 11720854 [ View in PubMed]
- Abstract
A series of PPARgamma agonists were synthesized from L-tyrosine that incorporated low molecular weight N-substituents. The most potent analogue, pyrrole (4e), demonstrated a K(i) of 6.9nM and an EC(50) of 4.7nM in PPARgamma 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.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Pioglitazone Peroxisome proliferator-activated receptor gamma EC 50 (nM) 580 N/A N/A Details Pioglitazone Peroxisome proliferator-activated receptor gamma Ki (nM) 630 N/A N/A Details Rosiglitazone Peroxisome proliferator-activated receptor gamma EC 50 (nM) 43 N/A N/A Details Rosiglitazone Peroxisome proliferator-activated receptor gamma Ki (nM) 120 N/A N/A Details