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

MA Massa, DP Spangler, RC Durley, BS Hickory…

Index: Massa, Mark A.; Spangler, Dale P.; Durley, Richard C.; Hickory, Brian S.; Connolly, Daniel T.; Witherbee, Bryan J.; Smith, Mark E.; Sikorski, James A. Bioorganic and Medicinal Chemistry Letters, 2001 , vol. 11, # 13 p. 1625 - 1628

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Citation Number: 36

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.