Design, synthesis, biological evaluation and docking studies of pterostilbene analogs inside PPARα

Pterostilbene, a naturally occurring analog of resveratrol, has previously shown PPAR alpha activation in H4IIEC3 cells and was found to decrease cholesterol levels in animals. In this study, analogs of pterostilbene were synthesized and their ability to activate PPARa was investigated. Among analogs that was synthesized (E)-4-(3,5-dimethoxystyryl) phenyl dihydrogen phosphate showed activity higher than pterostilbene and control drug ciprofibrate. Docking of the stilbenes inside PPARa showed the presence of important hydrogen bond interactions for PPAR alpha activation. (C) 2008 Elsevier Ltd. All rights reserved.