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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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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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creator	TOLLEFSON, Michael B KOLODZIEJ, Stephen A FLETCHER, Theresa R VERNIER, William F BEAUDRY, Judith A KELLER, Bradley T REITZ, David B
description	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.
doi_str_mv	10.1016/j.bmcl.2003.08.004
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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
title	A novel class of apical sodium co-dependent bile acid transporter inhibitors: The 1,2-benzothiazepines
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