Synthesis of novel β-propanamides to inhibit cholesteryl ester transfer protein (CETP)

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• 作者：Hong-Lei Xie ; Chun-Chi Liu ; Yi-Qun Li ; Chang-Lin Bai ; Chen-Zhou Hao ; Jing Guo ; Chang-Qun Luo ; Dong-Mei Zhao ; ^{medchemzhao@163.com} ; Mao-Sheng Cheng
• 关键词：CETP inhibitor ; Cardiovascular disease ; High-density lipoprotein ; Low-density lipoprotein ; In vitro
• 刊名：Chinese Chemical Letters
• 出版年：2017
• 出版时间：February 2017
• 年：2017
• 卷：28
• 期：2
• 页码：260-263
• 全文大小：884 K
• 卷排序：28

文摘

A novel series of β-propanamide derivatives as inhibitors of cholesteryl ester transfer protein (CETP) were synthesized. Previously, H3 (IC50 2 μmol/L) was observed to inhibit CETP moderately (Xie et al., 2016). Structural modifications based on H3 led to discovery of the successful CETP inhibitor, known as 1-methyl-4-arylpyrazole. Using a similar approach, compound Q08 was identified as a highly potent CETP inhibitor with an IC50 of 490 nmol/L in vitro.