Novel heteroaryl replacements of aromatic 3-tetrafluoroethoxy substituents in trifluoro-3-(tertiaryamino)-2-propanols as potent inhibitors of cholesteryl ester transfer protein. |
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| Authors: | M A Massa D P Spangler R C Durley B S Hickory D T Connolly B J Witherbee M E Smith J A Sikorski |
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| Institution: | Pharmacia Discovery Research, 700 Chesterfield Parkway North, 63198, St. Louis, MO, USA. massa@pharmacia.com |
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| 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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