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A new benzoxazine class of CETP inhibitors raises HDL cholesterol in transgenic mice and hamsters (Bioorg Med Chem Lett 2010)
Original title: Synthesis and discovery of 2,3-dihydro-3,8-diphenylbenzo[1,4]oxazines as a novel class of potent cholesteryl ester transfer protein inhibitors
2,3-Dihydro-3,8-diphenylbenzo[1,4]oxazines were identified as a new class of potent CETP inhibitors. The most potent compound, 6a, had an in vitro IC50 of 26 nanomolar, a favourable pharmacokinetic profile with 53% oral bioavailability in rats, and long human liver microsome stability (half-life of 62 minutes). Compound 6a increased HDL cholesterol both in human CETP transgenic mice and in high-fat-fed hamsters, and the paper details the structure-activity relationships underlying this series.
Original abstract
2,3-Dihydro-3,8-diphenylbenzo[1,4]oxazines were identified as a new class of potent cholesteryl ester transfer protein inhibitors. The most potent compound 6a (IC50=26 nM) possessed a favorable pharmacokinetic profile with good oral bioavailability in rat (F=53%) and long human liver microsome stability (t(1/2)=62 min). It increased HDL-C in human CETP transgenic mice and high-fat fed hamsters. The structure and activity relationship of this series will be described in this Letter.
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Summary written by cetpinhibition.org from the published abstract; figures as published. Page updated 19 August 2026. Methods.