title: Tetrazole and ester substituted tetrahydoquinoxalines as potent cholesteryl ester transfer protein inhibitors.
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.
authors.affiliation: Array BioPharma, 3200 Walnut Street Boulder, CO 80301, USA. teary@arraybiopharma.com
authors.forename: C Todd
authors.initials: CT
authors.lastname: Eary
authors.forename: Zachary S
authors.initials: ZS
authors.lastname: Jones
authors.forename: Robert D
authors.initials: RD
authors.lastname: Groneberg
authors.forename: Laurence E
authors.initials: LE
authors.lastname: Burgess
authors.forename: David A
authors.initials: DA
authors.lastname: Mareska
authors.forename: Mark D
authors.initials: MD
authors.lastname: Drew
authors.forename: James F
authors.initials: JF
authors.lastname: Blake
authors.forename: Ellen R
authors.initials: ER
authors.lastname: Laird
authors.forename: Devan
authors.initials: D
authors.lastname: Balachari
authors.forename: Michael
authors.initials: M
authors.lastname: O'Sullivan
authors.forename: Andrew
authors.initials: A
authors.lastname: Allen
authors.forename: Vivienne
authors.initials: V
authors.lastname: Marsh
mesh_terms: D000818:Animals; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D053480:Cholesterol Ester Transfer Proteins / Q000037:antagonists & inhibitors*; D008076:Cholesterol, HDL / Q000378:metabolism; D015195:Drug Design; D004952:Esters / Q000737:chemistry*; D006801:Humans; D006863:Hydrogen-Ion Concentration; D020128:Inhibitory Concentration 50; D008968:Molecular Conformation; D011810:Quinoxalines / Q000138:chemical synthesis* / Q000494:pharmacology*; D051381:Rats; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013777:Tetrazoles / Q000737:chemistry*
chemical_list: D053480:Cholesterol Ester Transfer Proteins; D008076:Cholesterol, HDL; D004952:Esters; D011810:Quinoxalines; D013777:Tetrazoles