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Tetrazole and ester substituted tetrahydoquinoxalines as potent cholesteryl ester transfer protein inhibitors
Authors:Eary C Todd  Jones Zachary S  Groneberg Robert D  Burgess Laurence E  Mareska David A  Drew Mark D  Blake James F  Laird Ellen R  Balachari Devan  O'Sullivan Michael  Allen Andrew  Marsh Vivienne
Affiliation:Array BioPharma, 3200 Walnut Street Boulder, CO 80301, USA. teary@arraybiopharma.com
Abstract:Cholesteryl ester transfer protein is a plasma glycoprotein that transfers cholesterol ester between lipoprotein particles. Inhibition of this protein, in vitro and in vivo, produces an increase in plasma high density lipoprotein cholesterol (HDL-C). This communication will describe the SAR and synthesis of a series of substituted tetrahydroquinoxaline CETP inhibitors from early mu lead to advanced enantiomerically pure analogs.
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