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

Abstract 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 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 IC 50 of 490 nmol/L in vitro .