Synthesis, Molecular Modeling and Biological Evaluation of Novel Trifluoromethyl Benzamides as Promising CETP Inhibitors


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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.

作者简介

Reema Abu Khalaf

Department of Pharmacy, Faculty of Pharmacy, Al-Zaytoonah University of Jordan

编辑信件的主要联系方式.
Email: info@benthamscience.net

Amani Abusaad

Department of Pharmacy, Faculty of Pharmacy, Al-Zaytoonah University of Jordan

Email: info@benthamscience.net

Bara'a Al-Nawaiseh

Department of Pharmacy, Al-Zaytoonah University of Jordan

Email: info@benthamscience.net

Dima Sabbah

Department of Pharmacy, Faculty of Pharmacy, Al-Zaytoonah University of Jordan

Email: info@benthamscience.net

Ghadeer Albadawi

Department of Pharmacy, Faculty of Pharmacy, Al-Zaytoonah University of Jordan

Email: info@benthamscience.net

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