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Molecules 2010, 15(8), 5721-5733; doi:10.3390/molecules15085721
Article

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

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Received: 18 June 2010 / Revised: 10 August 2010 / Accepted: 13 August 2010 / Published: 19 August 2010
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Abstract

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.
Keywords: CETP inhibitors; high-density lipoprotein; pharmacophore modeling; quantitative structure-activity relationship; benzylamino-methanones CETP inhibitors; high-density lipoprotein; pharmacophore modeling; quantitative structure-activity relationship; benzylamino-methanones
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Sheikha, G.A.; Abu Khalaf, R.; Melhem, A.; Albadawi, G. Design, Synthesis, and Biological Evaluation of Benzylamino-Methanone Based Cholesteryl Ester Transfer Protein Inhibitors. Molecules 2010, 15, 5721-5733.

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