Modifying the alpha-alkoxyamide moiety of arylbenzoxazole CETP inhibitors yields an orally bioavailable lead (Bioorg Med Chem Lett 2010)

Original title: 2-Arylbenzoxazoles as CETP inhibitors: substitution and modification of the alpha-alkoxyamide moiety

Bioorg Med Chem Lett · 16 December 2009 · 3

Hunt JA, Gonzalez S, Kallashi F, Hammond ML, Pivnichny JV, Tong X, Xu SS, Anderson MS, Chen Y, Eveland SS, Guo Q, Hyland SA et al.

This paper describes the development of a series of 2-arylbenzoxazole alpha-alkoxyamide and beta-alkoxyamine CETP inhibitors. Highly fluorinated alpha-alkoxyamides proved to be potent CETP inhibitors in vitro, and the highly fluorinated 2-arylbenzoxazole beta-alkoxyamine compound 4 showed a desirable combination of in vitro potency (IC50 equals 151 nanomolar) and oral bioavailability in mice.

Original abstract

The development of a series of 2-arylbenzoxazole alpha-alkoxyamide and beta-alkoxyamine inhibitors of cholesteryl ester transfer protein (CETP) is described. Highly fluorinated alpha-alkoxyamides proved to be potent inhibitors of CETP in vitro, and the highly fluorinated 2-arylbenzoxazole beta-alkoxyamine 4 showed a desirable combination of in vitro potency (IC(50)=151 nM) and oral bioavailability in the mouse.

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