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Bioorg Med Chem Lett. 2003 Nov 3;13(21):3727-30.

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

Author information

1
Pfizer Global Research and Development, 700 Chesterfield Parkway N, Chesterfield, MO 63017, USA. michael.b.tollefson@pfizer.com

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.

PMID:
14552767
DOI:
10.1016/j.bmcl.2003.08.004
[Indexed for MEDLINE]

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