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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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* ,
 and
Department of Pharmaceutical Sciences, Faculty of Pharmacy, Al-Zaytoonah Private University of Jordan, Amman, Jordan
* Author to whom correspondence should be addressed.
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 (CC BY 3.0).
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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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