Discovery of a simple picomolar inhibitor of cholesteryl ester transfer protein

…, ML Grapperhaus, BS Hickory, MA Massa…

Index: Reinhard, Emily J.; Wang, Jane L.; Durley, Richard C.; Fobian, Yvette M.; Grapperhaus, Margaret L.; Hickory, Brian S.; Massa, Mark A.; Norton, Monica B.; Promo, Michele A.; Tollefson, Michael B.; Vernier, William F.; Connolly, Daniel T.; Witherbee, Bryan J.; Melton, Michele A.; Regina, Karen J.; Smith, Mark E.; Sikorski, James A. Journal of Medicinal Chemistry, 2003 , vol. 46, # 11 p. 2152 - 2168

Full Text: HTML

Citation Number: 43

Abstract

A novel series of substituted N-[3-(1, 1, 2, 2-tetrafluoroethoxy) benzyl]-N-(3-phenoxyphenyl)- trifluoro-3-amino-2-propanols is described which potently and reversibly inhibit cholesteryl ester transfer protein (CETP). Starting from the initial lead 1, various substituents were introduced into the 3-phenoxyaniline group to optimize the relative activity for inhibition of the CETP-mediated transfer of [3H]-cholesteryl ester from HDL donor particles to LDL ...