Design, Synthesis and Biological Evaluation of some Chalcone Derivatives as Potential Pancreatic Lipase Inhibitors

Obesity is a growing global health problem, but few drugs are available for the treatment of obesity. Several classes of compounds have been studied and demonstrated for the human lipase inhibition activity - a target in obesity prevention. This study was about design, synthesis and biological evaluation of some synthetic chalcones as pancreatic lipase inhibitors. FlexX software integrated in LeadIT was used for molecular docking studies of 66 chalcone derivatives. 6 derivatives with low docking scores (good binding affinity) were selected for synthesis using both classical and microwave-assisted Claisen-Schmidt condensation reactions. Biological evaluation on pancreatic lipase indicated that some chalcones showed good lipase inhibition activities and that there were correlations between in silico model and biological activities. These presented the possibility to apply virtual screening tools in finding potential agents with high obesity-prevention capacity. Keywords: lipase inhibitory activity, chalcone,