Benzamides as CETP Inhibitors

What is it about?

Herein, synthesis and characterization of ten benzyl benzamides 8a-j that aim at CETP inhibition was performed. In vitro CETP inhibition bioassay revealed that benzamide 8j had the best activity with a percent inhibition of 82.2% at 10 µM concentration and an IC50 of 1.3 µM. Docking study shows that the verified compounds accommodate the binding cleft of CETP and are enclosed by hydrophobic lining. Furthermore, the scaffold of 8a-j matches the pharmacophoric points of CETP inhibitors; particularly hydrophobic and aromatic functionalities.

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Why is it important?

Cardiovascular disease is the most common cause for mortality and morbidity in the developed world, which risk is inversely related to the HDL cholesterol levels. Therefore, there is a great interest in developing new CETP inhibitors capable of raising HDL as a novel approach for prevention of cardiovascular disease.