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Arylsulfonylamino-Benzanilides as Inhibitors of the Apical Sodium-Dependent Bile Salt Transporter (SLC10A2)
The apical sodium-dependent bile salt transporter (ASBT) plays a pivotal role in maintaining bile acid homeostasis. Inhibition of ASBT would reduce bile acid pool size and lower cholesterol levels. In this report, a series of novel arylsulfonylaminobenzanilides were designed and synthesized as poten...
| Autores principales: | , , , , , , , |
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| Formato: | Online Artículo Texto |
| Lenguaje: | English |
| Publicado: |
MDPI
2013
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| Materias: | |
| Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6269792/ https://www.ncbi.nlm.nih.gov/pubmed/23752471 http://dx.doi.org/10.3390/molecules18066883 |
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| author | Liu, Hong-Tao He, Hong-Wei Bai, Xiao-Guang Wang, Ju-Xian Xu, Chang-Liang Cai, Shi-Ying Shao, Rong-Guang Wang, Yu-Cheng |
| author_facet | Liu, Hong-Tao He, Hong-Wei Bai, Xiao-Guang Wang, Ju-Xian Xu, Chang-Liang Cai, Shi-Ying Shao, Rong-Guang Wang, Yu-Cheng |
| author_sort | Liu, Hong-Tao |
| collection | PubMed |
| description | The apical sodium-dependent bile salt transporter (ASBT) plays a pivotal role in maintaining bile acid homeostasis. Inhibition of ASBT would reduce bile acid pool size and lower cholesterol levels. In this report, a series of novel arylsulfonylaminobenzanilides were designed and synthesized as potential inhibitors of ASBT. Most of them demonstrated great potency against ASBT’s bile acid transport activity. In particular, compound 5g(2) inhibited ASBT activity with an IC(50) value of 0.11 μM. These compounds represent potential cholesterol-lowering drugs. |
| format | Online Article Text |
| id | pubmed-6269792 |
| institution | National Center for Biotechnology Information |
| language | English |
| publishDate | 2013 |
| publisher | MDPI |
| record_format | MEDLINE/PubMed |
| spelling | pubmed-62697922018-12-17 Arylsulfonylamino-Benzanilides as Inhibitors of the Apical Sodium-Dependent Bile Salt Transporter (SLC10A2) Liu, Hong-Tao He, Hong-Wei Bai, Xiao-Guang Wang, Ju-Xian Xu, Chang-Liang Cai, Shi-Ying Shao, Rong-Guang Wang, Yu-Cheng Molecules Article The apical sodium-dependent bile salt transporter (ASBT) plays a pivotal role in maintaining bile acid homeostasis. Inhibition of ASBT would reduce bile acid pool size and lower cholesterol levels. In this report, a series of novel arylsulfonylaminobenzanilides were designed and synthesized as potential inhibitors of ASBT. Most of them demonstrated great potency against ASBT’s bile acid transport activity. In particular, compound 5g(2) inhibited ASBT activity with an IC(50) value of 0.11 μM. These compounds represent potential cholesterol-lowering drugs. MDPI 2013-06-10 /pmc/articles/PMC6269792/ /pubmed/23752471 http://dx.doi.org/10.3390/molecules18066883 Text en © 2013 by the authors; licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/). |
| spellingShingle | Article Liu, Hong-Tao He, Hong-Wei Bai, Xiao-Guang Wang, Ju-Xian Xu, Chang-Liang Cai, Shi-Ying Shao, Rong-Guang Wang, Yu-Cheng Arylsulfonylamino-Benzanilides as Inhibitors of the Apical Sodium-Dependent Bile Salt Transporter (SLC10A2) |
| title | Arylsulfonylamino-Benzanilides as Inhibitors of the Apical Sodium-Dependent Bile Salt Transporter (SLC10A2) |
| title_full | Arylsulfonylamino-Benzanilides as Inhibitors of the Apical Sodium-Dependent Bile Salt Transporter (SLC10A2) |
| title_fullStr | Arylsulfonylamino-Benzanilides as Inhibitors of the Apical Sodium-Dependent Bile Salt Transporter (SLC10A2) |
| title_full_unstemmed | Arylsulfonylamino-Benzanilides as Inhibitors of the Apical Sodium-Dependent Bile Salt Transporter (SLC10A2) |
| title_short | Arylsulfonylamino-Benzanilides as Inhibitors of the Apical Sodium-Dependent Bile Salt Transporter (SLC10A2) |
| title_sort | arylsulfonylamino-benzanilides as inhibitors of the apical sodium-dependent bile salt transporter (slc10a2) |
| topic | Article |
| url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6269792/ https://www.ncbi.nlm.nih.gov/pubmed/23752471 http://dx.doi.org/10.3390/molecules18066883 |
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