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

Bioorganic & Medicinal Chemistry Letters
Cameron J SmithPeter J Sinclair

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.

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Citations

Jan 6, 2012·Chemical Communications : Chem Comm·Fabrizio CartaClaudiu T Supuran
Dec 1, 2010·Expert Opinion on Drug Discovery·Yuan YangBin Hong
Oct 26, 2016·Journal of the American Chemical Society·Bethany G CaulkinsLeonard J Mueller
Apr 19, 2017·Journal of the American Chemical Society·Xiaoming WangFrank Glorius
Jul 30, 2019·Journal of Computational Biology : a Journal of Computational Molecular Cell Biology·Wilson Alberto TárragaMarina Cecilia Gonzalez
Oct 24, 2013·Organic Letters·Jörg SedelmeierFrancesco Venturoni
Mar 25, 2020·Organic Letters·Sourav Sekhar Bera, Modhu Sudan Maji

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