title: Novel heteroaryl replacements of aromatic 3-tetrafluoroethoxy substituents in trifluoro-3-(tertiaryamino)-2-propanols as potent inhibitors of cholesteryl ester transfer protein.
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.
authors: Pharmacia Discovery Research, 700 Chesterfield Parkway North, 63198, St. Louis, MO, USA. massa@pharmacia.com
authors: M A
authors: MA
authors: Massa
authors: D P
authors: DP
authors: Spangler
authors: R C
authors: RC
authors: Durley
authors: B S
authors: BS
authors: Hickory
authors: D T
authors: DT
authors: Connolly
authors: B J
authors: BJ
authors: Witherbee
authors: M E
authors: ME
authors: Smith
authors: J A
authors: JA
authors: Sikorski
mesh_terms: D002352:Carrier Proteins / Q000037:antagonists & inhibitors*; D053480:Cholesterol Ester Transfer Proteins; D006023:Glycoproteins; D020005:Propanols / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D002352:Carrier Proteins; D053480:Cholesterol Ester Transfer Proteins; D006023:Glycoproteins; D020005:Propanols