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


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 ?M) in vitro and showed an acceptable metabolic stability.

SUBMITTER: Wang X 

PROVIDER: S-EPMC6150381 | biostudies-literature | 2017 Nov

REPOSITORIES: biostudies-literature

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

Wang Xinran X   Lin Xuehua X   Xu Xuanqi X   Li Wei W   Hao Lijuan L   Liu Chunchi C   Zhao Dongmei D   Cheng Maosheng M  

Molecules (Basel, Switzerland) 20171107 11


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 <b>5</b> was discovered as a moderate CETP inhibitor. The replacement of the amide linker by heterocyclic aromatics and then a series of <i>N</i>,<i>N</i>-substituted-4-arylthiazole-2-methylamine derivatives were designed by utilizing a conformational restriction strategy. Thir  ...[more]

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