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

作者：Wang, Xinran; Hao, Lijuan; Xu, Xuanqi; Li, Wei; Liu, Chunchi; Zhao, Dongmei^*; Cheng, Maosheng

来源：Molecules, 2017, 22(10): 1658.

DOI：10.3390/molecules22101658

• synthesis
• N,N-substituted amine derivatives
• CETP inhibitors
• HDL-C

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 mu M) in vitro. Furthermore, compound 17 was selected for an in vitro metabolic stability study.

• 出版日期2017-10
• 单位沈阳药科大学