Design, synthesis, and evaluation of novel aryl-tetrahydropyridine PPARalpha/gamma dual agonists.

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Kim E, Park CS, Han T, Bae MH, Chong W, Lee CH, Shin YA, Ahn BN, Kim MK, Shin CY, Son MH, Kim JK, Moon HS, Shim HJ, Kim EJ, Kim SH, Lim JI, Lee CH

Design, synthesis, and evaluation of novel aryl-tetrahydropyridine PPARalpha/gamma dual agonists.

Bioorg Med Chem Lett. 2008 Sep 15;18(18):4993-6. doi: 10.1016/j.bmcl.2008.08.020. Epub 2008 Aug 12.

PubMed ID
18771917 [ View in PubMed
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Abstract

Aryl-tetrahydropyridine derivatives were prepared and their PPARalpha/gamma dual agonistic activities were evaluated. Among them, compound (S)-5b was identified as a potent PPARalpha/gamma dual agonist with an EC(50) of 1.73 and 0.64 microM in hPPARalpha and gamma, respectively. In diabetic (db/db) mice, compound (S)-5b showed good glucose lowering efficacy and favorable pharmacokinetic properties.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
RosiglitazonePeroxisome proliferator-activated receptor alphaEC 50 (nM)3460N/AN/ADetails
RosiglitazonePeroxisome proliferator-activated receptor gammaEC 50 (nM)33N/AN/ADetails
TesaglitazarPeroxisome proliferator-activated receptor alphaEC 50 (nM)3120N/AN/ADetails
TesaglitazarPeroxisome proliferator-activated receptor gammaEC 50 (nM)704N/AN/ADetails