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）.S...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.展开更多
基金supported by the National Natural Science Foundation of China (No. 81373324)the program for Innovative Research Team of the Ministry of Education and Program for Liaoning Innovative Research Team in University
文摘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.
