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Molecules 2017, 22(11), 1925; doi:10.3390/molecules22111925

Design, Synthesis, and Biological Evaluation of N,N-Disubstituted-4-Arylthiazole-2-Methylamine Derivatives as Cholesteryl Ester Transfer Inhibitors

1
Key Laboratory of Structure-Based Drug Design & Discovery of Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, China
2
Department of Chemistry, University of Wisconsin-Madison, Madison, WI 53715, USA
These authors contributed equally to this work.
*
Author to whom correspondence should be addressed.
Received: 15 October 2017 / Accepted: 27 October 2017 / Published: 7 November 2017
(This article belongs to the Section Medicinal Chemistry)
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Abstract

Cholesteryl ester transfer protein (CETP) has been identified as a potential target for cardiovascular disease (CVD) for its important role in the reverse cholesteryl transfer (RCT) process. In our previous work, compound 5 was discovered as a moderate CETP inhibitor. The replacement of the amide linker by heterocyclic aromatics and then a series of N,N-substituted-4-arylthiazole-2-methylamine derivatives were designed by utilizing a conformational restriction strategy. Thirty-six compounds were synthesized and evaluated for their CETP inhibitory activities. Structure-activity relationship studies indicate that electron donor groups substituted ring A, and electron-withdrawing groups at the 4-position of ring B were critical for potency. Among these compounds, compound 30 exhibited excellent CETP inhibitory activity (IC50 = 0.79 ± 0.02 μM) in vitro and showed an acceptable metabolic stability. View Full-Text
Keywords: synthesis; N,N-disubstituted-4-arylthiazole-2-methylamine derivatives; CETP inhibitors synthesis; N,N-disubstituted-4-arylthiazole-2-methylamine derivatives; CETP inhibitors
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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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MDPI and ACS Style

Wang, X.; Lin, X.; Xu, X.; Li, W.; Hao, L.; Liu, C.; Zhao, D.; Cheng, M. Design, Synthesis, and Biological Evaluation of N,N-Disubstituted-4-Arylthiazole-2-Methylamine Derivatives as Cholesteryl Ester Transfer Inhibitors. Molecules 2017, 22, 1925.

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