A novel class of apical sodium co-dependent bile acid transporter inhibitors: The 1,2-benzothiazepines

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 acti...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2003-11, Vol.13 (21), p.3727-3730
Main Authors: TOLLEFSON, Michael B, KOLODZIEJ, Stephen A, FLETCHER, Theresa R, VERNIER, William F, BEAUDRY, Judith A, KELLER, Bradley T, REITZ, David B
Format: Article
Language:English
Subjects:
Animals
Biological and medical sciences
Cell Line
Cricetinae
Electrons
General and cellular metabolism. Vitamins
Humans
Hypolipidemic Agents - chemical synthesis
Hypolipidemic Agents - pharmacology
Indicators and Reagents
Medical sciences
Organic Anion Transporters, Sodium-Dependent - antagonists & inhibitors
Oxidation-Reduction
Pharmacology. Drug treatments
Polyethylene Glycols
Symporters - antagonists & inhibitors
Thiazepines - chemical synthesis
Thiazepines - pharmacology
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Summary: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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2003.08.004