2-Arylbenzoxazole CETP inhibitors raise HDL cholesterol in cynoCETP transgenic mice (Bioorg Med Chem Lett 2011)

Original title: 2-Arylbenzoxazoles as CETP inhibitors: raising HDL-C in cynoCETP transgenic mice

Bioorg Med Chem Lett · 20 October 2010 · 4

Kallashi F, Kim D, Kowalchick J, Park YJ, Hunt JA, Ali A, Smith CJ, Hammond ML, Pivnichny JV, Tong X, Xu SS, Anderson MS et al.

Structure-activity studies led to the discovery of 2-arylbenzoxazole compound 3, the first in a series shown to raise serum HDL cholesterol in transgenic mice expressing cynomolgus CETP. Replacing the 4-piperidinyloxy moiety with a piperazinyl group gave a more synthetically tractable lead, and further optimisation produced compound 4, described as an excellent inhibitor of CETP function with good pharmacokinetic properties and in vivo efficacy.

Original abstract

We describe structure-activity studies leading to the discovery of 2-arylbenzoxazole 3, the first in a series to raise serum high-density lipoprotein cholesterol levels in transgenic mice. Replacement of the 4-piperidinyloxy moiety with piperazinyl provided a more synthetically tractable lead, which upon optimization resulted in compound 4, an excellent inhibitor of cholesteryl ester transfer protein function with good pharmacokinetic properties and in vivo efficacy.

Summary written by cetpinhibition.org from the published abstract; figures as published. Page updated 19 August 2026. Methods.