Synthesis and evaluation of aminomethyl dihydrocinnamates as a new class of PPAR ligands.

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Warshawsky AM, Alt CA, Brozinick JT, Harkness AR, Hawkins ED, Henry JR, Matthews DP, Miller AR, Misener EA, Montrose-Rafizadeh C, Rhodes GA, Shen Q, Vance JA, Udodong UE, Wang M, Zhang TY, Zink RW

Synthesis and evaluation of aminomethyl dihydrocinnamates as a new class of PPAR ligands.

Bioorg Med Chem Lett. 2006 Dec 15;16(24):6328-33. Epub 2006 Sep 26.

PubMed ID
17005394 [ View in PubMed
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Abstract

PPAR ligands with varied subtype selectivity have been synthesized using an achiral aminomethyl dihydrocinnamate template. Several compounds in this series have demonstrated potent plasma glucose and triglyceride lowering capability in rodent models of type 2 diabetes.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
RosiglitazonePeroxisome proliferator-activated receptor alphaIC 50 (nM)>10000N/AN/ADetails
RosiglitazonePeroxisome proliferator-activated receptor gammaEC 50 (nM)308N/AN/ADetails
RosiglitazonePeroxisome proliferator-activated receptor gammaIC 50 (nM)67N/AN/ADetails