Synthesis, molecular docking and evaluation of hypolipidemic activities of novel benzophenonecarboxamide derivatives

摘要

Fibrates are well known hypolipidemic agents and act by activating Peroxisome Proliferator-Activated Receptors (PPAR); this family of receptors is the main regulator for fatty acid metabolism. In the present study, a total of six novel benzophenonecarboxamide derivatives (3-6, 9 and 10) have been synthesized and evaluated for their hypolipidemic activity. Interestingly, compounds 4 and 6 show promising hypolipidemic activity and lower the level of TG by 71% and LDL-C by 26% and 29% respectively. Further, molecular docking studies have been carried out to gain insight into the binding interactions of all the newly synthesized compounds inside the PPAR alpha receptor and the results are in consonance with the biological activity. The encouraging in vivohypolipidemic activity of compounds 4 and 6 by lowering LDL-C levels as well as enhancing HDL-C indicates that these compounds can serve as promising lead compounds for further investigations for the development of novel hypolipidemic agents.