Literature DB >> 14552767

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

Michael B Tollefson1, Stephen A Kolodziej, Theresa R Fletcher, William F Vernier, Judith A Beaudry, Bradley T Keller, David B Reitz.   

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.

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Year:  2003        PMID: 14552767     DOI: 10.1016/j.bmcl.2003.08.004

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  6 in total

1.  The Concise Guide to PHARMACOLOGY 2013/14: transporters.

Authors:  Stephen P H Alexander; Helen E Benson; Elena Faccenda; Adam J Pawson; Joanna L Sharman; Michael Spedding; John A Peters; Anthony J Harmar
Journal:  Br J Pharmacol       Date:  2013-12       Impact factor: 8.739

Review 2.  Role of the intestinal bile acid transporters in bile acid and drug disposition.

Authors:  Paul A Dawson
Journal:  Handb Exp Pharmacol       Date:  2011

3.  Inhibition of ileal bile acid uptake protects against nonalcoholic fatty liver disease in high-fat diet-fed mice.

Authors:  Anuradha Rao; Astrid Kosters; Jamie E Mells; Wujuan Zhang; Kenneth D R Setchell; Angelica M Amanso; Grace M Wynn; Tianlei Xu; Brad T Keller; Hong Yin; Sophia Banton; Dean P Jones; Hao Wu; Paul A Dawson; Saul J Karpen
Journal:  Sci Transl Med       Date:  2016-09-21       Impact factor: 17.956

4.  A novel class of apical sodium--dependent bile salt transporter inhibitors: 1-(2,4-bifluorophenyl)-7-dialkylamino-1,8-naphthyridine-3-carboxamides.

Authors:  Hongtao Liu; Guoxun Pang; Jinfeng Ren; Yue Zhao; Juxian Wang
Journal:  Acta Pharm Sin B       Date:  2016-12-23       Impact factor: 11.413

5.  Ni(II)-catalyzed asymmetric alkenylations of ketimines.

Authors:  Mao Quan; Xiaoxiao Wang; Liang Wu; Ilya D Gridnev; Guoqiang Yang; Wanbin Zhang
Journal:  Nat Commun       Date:  2018-06-08       Impact factor: 14.919

6.  A Scaffold-Diversity Synthesis of Biologically Intriguing Cyclic Sulfonamides.

Authors:  Stefan Zimmermann; Mohammad Akbarzadeh; Felix Otte; Carsten Strohmann; Muthukumar Gomathi Sankar; Slava Ziegler; Axel Pahl; Sonja Sievers; Kamal Kumar
Journal:  Chemistry       Date:  2019-11-07       Impact factor: 5.236

  6 in total

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