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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

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
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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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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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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