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Molecules 2017, 22(10), 1658; doi:10.3390/molecules22101658

Design, Synthesis and Biological Evaluation of N,N-Substituted Amine Derivatives as Cholesteryl Ester Transfer Protein Inhibitors

Key Laboratory of Structure-Based Drug Design & Discovery of Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, China
Department of Chemistry, University of Wisconsin-Madison, Madison, WI, 53715, USA
Author to whom correspondence should be addressed.
Received: 20 August 2017 / Revised: 29 September 2017 / Accepted: 30 September 2017 / Published: 3 October 2017
(This article belongs to the Section Medicinal Chemistry)
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N,N-Substituted amine derivatives were designed by utilizing a bioisosterism strategy. Consequently, twenty-two compounds were synthesized and evaluated for their inhibitory activity against CETP. Structure-activity relationship (SAR) studies indicate that hydrophilic groups at the 2-position of the tetrazole and 3,5-bistrifluoromethyl groups on the benzene ring provide important contributions to the potency. Among these compounds, compound 17 exhibited excellent CETP inhibitory activity (IC50 = 0.38 ± 0.08 μM) in vitro. Furthermore, compound 17 was selected for an in vitro metabolic stability study. View Full-Text
Keywords: synthesis; N,N-substituted amine derivatives; CETP inhibitors; HDL-C synthesis; N,N-substituted amine derivatives; CETP inhibitors; HDL-C

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. (CC BY 4.0).

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Wang, X.; Hao, L.; Xu, X.; Li, W.; Liu, C.; Zhao, D.; Cheng, M. Design, Synthesis and Biological Evaluation of N,N-Substituted Amine Derivatives as Cholesteryl Ester Transfer Protein Inhibitors. Molecules 2017, 22, 1658.

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