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