Design, Synthesis, and Biological Evaluation of Benzylamino-Methanone Based Cholesteryl Ester Transfer Protein Inhibitors

Molecules

Ghassan Abu Sheikha¹  Reema Abu Khalaf¹  Areej Melhem¹ 

[1] Department of Pharmaceutical Sciences, Faculty of Pharmacy, Al-Zaytoonah Private University of Jordan, Amman, Jordan

关键词: CETP inhibitors;    high-density lipoprotein;    pharmacophore modeling;    quantitative structure-activity relationship;    benzylamino-methanones;   

DOI  :  10.3390/molecules15085721

来源: mdpi

【 摘 要 】

Cholesteryl ester transfer protein (CETP) is a glycoprotein involved in transporting lipoprotein particles and neutral lipids between high-density lipoprotein (HDL) and low density lipoproteins (LDL) and therefore its a proper target for treating dyslipidemia and related disorders. Guided by our previosuly-reported pharmacophore and QSAR models for CETP inhibition, we synthesized and bioassayed a series of benzylamino-methanones. The most potent illustrated 30% CETP inhibition at 10 μM.

【 授权许可】

CC BY   
This is an open access article distributed under the Creative Commons Attribution License (CC BY) which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.