【摘 要】
：
A novel series of β-propanamide derivatives as inhibitors of cholesteryl ester transfer protein(CETP)were synthesized.Previously,H3(IC_(50) 2 μmol/L) was obse
【机 构】
：
Key Laboratory of Structure-Based Drug Design and Discovery of Ministry of Education, Shenyang Pharm
【出 处】
：
Chinese Chemical Letters
论文部分内容阅读
A novel series of β-propanamide derivatives as inhibitors of cholesteryl ester transfer protein(CETP)were synthesized.Previously,H3(IC_(50) 2 μmol/L) was observed to inhibit CETP moderately(Xie et ah,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 IC_(50) of 490 nmol/L in vitro.
A novel series of β-propanamide derivatives as inhibitors of cholesteryl ester transfer protein (CETP) were synthesized. Previously, H3 (IC 50 (2 μmol / L) was observed to inhibit CETP moderately (Xie et ah, 2016) 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 IC 50 of 490 nmol / L in vitro .
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