title: A novel class of apical sodium co-dependent bile acid transporter inhibitors: the 1,2-benzothiazepines.
abstract: A series of 5-aryl-3,3-dibutyl-7-(dimethylamino)-1,2-benzothiazepin-4-ol 1,1-dioxides were prepared and were found to inhibit the apical sodium co-dependent bile acid transporter (ASBT) for the potential treatment for hyperlipidemia. Several 1,2-benzothiazepines exhibited low nanomolar in vitro activity. The synthesis and initial in vitro potency data is presented for this novel class of compounds.
authors.affiliation: Pfizer Global Research and Development, 700 Chesterfield Parkway N, Chesterfield, MO 63017, USA. michael.b.tollefson@pfizer.com
authors.forename: Michael B
authors.initials: MB
authors.lastname: Tollefson
authors.forename: Stephen A
authors.initials: SA
authors.lastname: Kolodziej
authors.forename: Theresa R
authors.initials: TR
authors.lastname: Fletcher
authors.forename: William F
authors.initials: WF
authors.lastname: Vernier
authors.forename: Judith A
authors.initials: JA
authors.lastname: Beaudry
authors.forename: Bradley T
authors.initials: BT
authors.lastname: Keller
authors.forename: David B
authors.initials: DB
authors.lastname: Reitz
mesh_terms: D000818:Animals; D002460:Cell Line; D006224:Cricetinae; D004583:Electrons; D006801:Humans; D000960:Hypolipidemic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D007202:Indicators and Reagents; D029363:Organic Anion Transporters, Sodium-Dependent / Q000037:antagonists & inhibitors*; D010084:Oxidation-Reduction; D011092:Polyethylene Glycols; D027981:Symporters / Q000037:antagonists & inhibitors*; D013841:Thiazepines / Q000138:chemical synthesis* / Q000494:pharmacology*
chemical_list: D000960:Hypolipidemic Agents; D007202:Indicators and Reagents; D029363:Organic Anion Transporters, Sodium-Dependent; D027981:Symporters; D013841:Thiazepines; C071908:sodium-bile acid cotransporter; D011092:Polyethylene Glycols