Lipase inhibitory activity

Pancreatic lipase is one of the safest targets of anti-obesity drugs. To date, orlistat is the only pancreatic lipase inhibitor approved for the long-term treatment of obesity. Therefore, there is an elevated need to find new drugs for this disease. Determining the factors affecting the test to evaluate pancreatic lipase inhibitory activity in order to build a standard assay procedure is necessary. This will make it much easier for researchers to find novel compounds that inhibit the enzyme.

6p viwolverine 07-07-2023 7 1   Download

Twenty-five new hydroxy- and methoxy-substituted 4,6-diarylpyrimidin-2(1H)-ol (20–34) and 4,6-diarylpyrimidine-2(1H)-thiol derivatives (35–44) were synthesized from the reaction of the corresponding 1,3-diaryl-2-propene-1- one compounds (1–19) with urea or thiourea using the solid-phase microwave method. All the new synthetic compounds (20–44) were evaluated with regard to their α-glucosidase activity. However, only compounds 22–25, 27, 31, 34, 35, 37, and 40 exhibited a greater inhibitory effect than standard acarbose. The IC50 values of the active compounds ranged between 2.36 and 13.

16p tudichquannguyet 29-11-2021 9 1   Download

This study focused on benzyl amino chalcone derivatives as they have a benzyl group that can mimic the hydrophobic effect of the long chain carbon of Orlistat, a drug used to treat obesity. Initially, 102 molecular structures were prepared and docked into the protein by using AutoDock Vina version 1.5.6. Fourteen structures having good docking scores were selected to synthesize using a ClaisenSchmidt reaction.

11p nguyenmyhuyen90 04-03-2021 9 2   Download