Citation: Xie Hong-Lei, Liu Chun-Chi, Li Yi-Qun, Bai Chang-Lin, Hao Chen-Zhou, Guo Jing, Luo Chang-Qun, Zhao Dong-Mei, Cheng Mao-Sheng. Synthesis of novel β-propanamides to inhibit cholesteryl ester transfer protein (CETP)[J]. Chinese Chemical Letters, ;2017, 28(2): 260-263. doi: 10.1016/j.cclet.2016.10.016 shu

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

Key Laboratory of Structure-Based Drug Design and Discovery of Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, China

Corresponding author: Zhao Dong-Mei, medchemzhao@163.com
Received Date: 6 June 2016
Revised Date: 9 August 2016
Accepted Date: 9 August 2016
Available Online: 21 February 2016

Figures(2)

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.
- CETP inhibitor,
- Cardiovascular disease,
- High-density lipoprotein,
- Low-density lipoprotein,
- In vitro
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