LAUSR

BACKGROUND Hyperlipidemia is considered a major risk factor for the progress of atherosclerosis. OBJECTIVE Cholesteryl ester transfer protein (CETP) facilitates the relocation of cholesterol esters from HDL to LDL. CETP inhibition produces higher HDL and lower LDL levels. METHODS Synthesis of nine benzylamino benzamides 8a-8f and 9a-9c was performed. RESULTS In vitro biological study displayed potential CETP inhibitory activity, where compound 9c had the best activity with an IC50 of 1.03 µM. Induced-fit docking demonstrated that 8a-8f and 9a-9c accommodated the CETP active site and hydrophobic interaction predominated ligand/ CETP complex formation. CONCLUSION Pharmacophore mapping showed that this scaffold endorsed CETP inhibitors features and consequently elaborated the high CETP binding affinity.