Lead 2-arylbenzoxazole compound inhibits CETP with an IC50 of 28 nanomolar (Bioorg Med Chem Lett 2009)

Original title: 2-Arylbenzoxazoles as CETP inhibitors: Substitution of the benzoxazole moiety

Bioorg Med Chem Lett · 29 October 2009 · 4

Smith CJ, Ali A, Chen L, Hammond ML, Anderson MS, Chen Y, Eveland SS, Guo Q, Hyland SA, Milot DP, Sparrow CP, Wright SD et al.

Medicinal chemists describe a series of 2-arylbenzoxazole inhibitors of cholesteryl ester transfer protein, with structure-activity studies focused on varying the substitution pattern of the benzoxazole moiety. Substitution at the 5- and 7-positions proved beneficial for CETP inhibition, and the most potent compound in the series, compound 47, inhibited CETP with an IC50 of 28 nanomolar, establishing benzoxazole substitution as a productive avenue for optimizing this inhibitor class.

Original abstract

A series of 2-arylbenzoxazole inhibitors of the cholesterol ester transfer protein (CETP) is described. Structure-activity studies focused on variation of the substitution of the benzoxazole moiety. Substitution at the 5- and 7-positions of the benzoxazole moiety was found to be beneficial for CETP inhibition. Compound 47 was found to be the most potent inhibitor in this series and inhibited CETP with an IC(50) of 28nM.

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