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Replacing a tetrafluoroethoxy group with 2-furyl heteroaryl moieties yields submicromolar CETP inhibitors in a new trifluoro-propanol series (Bioorg Med Chem Lett 2001)

Original title: Novel heteroaryl replacements of aromatic 3-tetrafluoroethoxy substituents in trifluoro-3-(tertiaryamino)-2-propanols as potent inhibitors of cholesteryl ester transfer protein

Bioorg Med Chem Lett · · 5

Massa MA, Spangler DP, Durley RC, Hickory BS, Connolly DT, Witherbee BJ, Smith ME, Sikorski JA

The authors prepared a series of novel N,N-disubstituted trifluoro-3-amino-2-propanols as potent inhibitors of cholesteryl ester transfer protein (CETP). Modifying the aromatic 3-tetrafluoroethoxy group in the lead molecule 1a with various heteroaryl moieties produced new 2-furyl analogues, compounds 2a and 2b, which showed submicromolar potency in vitro.

Read the paper (DOI)PubMed

Original abstract

A series of novel N,N-disubstituted trifluoro-3-amino-2-propanols has been prepared as potent inhibitors of cholesteryl ester transfer protein (CETP). Modifying the aromatic 3-tetrafluoroethoxy group in the lead molecule 1a with various heteroaryl moieties produced new 2-furyl analogues 2a,b with submicromolar potency in vitro.

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