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ID: ALA1136319

Journal: Bioorg Med Chem Lett

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

Authors: Tollefson MB, Kolodziej SA, Fletcher TR, Vernier WF, Beaudry JA, Keller BT, Reitz DB.

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.

CiteXplore: 14552767

DOI: 10.1016/j.bmcl.2003.08.004