2-Arylbenzoxazoles as CETP inhibitors: Substitution and modification of the α-alkoxyamide moiety

The development of a series of 2-arylbenzoxazole α-alkoxyamide and β-alkoxyamine inhibitors of cholesteryl ester transfer protein (CETP) is described. Highly fluorinated α-alkoxyamides proved to be potent inhibitors of CETP in vitro, and the highly fluorinated 2-arylbenzoxazole β-alkoxyamine 4 showed a desirable combination of in vitro potency (IC50 = 151 nM) and oral bioavailability in the mouse.

Graphical abstractCompound 4 was found to be a potent (IC50 = 151 nM) and orally bioavailable inhibitor of CETP.Figure optionsDownload full-size imageDownload as PowerPoint slide