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Molecules 2013, 18(6), 6883-6897; doi:10.3390/molecules18066883
Article

Arylsulfonylamino-Benzanilides as Inhibitors of the Apical Sodium-Dependent Bile Salt Transporter (SLC10A2)

1, 1, 1, 1, 1, 2, 1,*  and 1,*
Received: 2 May 2013 / Revised: 4 June 2013 / Accepted: 5 June 2013 / Published: 10 June 2013
(This article belongs to the Section Medicinal Chemistry)
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Abstract

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 5g2 inhibited ASBT activity with an IC50 value of 0.11 μM. These compounds represent potential cholesterol-lowering drugs.
Keywords: ASBT inhibitors; bile acids; arylsulfonylaminobenzanilides; cholesterol lowering drug ASBT inhibitors; bile acids; arylsulfonylaminobenzanilides; cholesterol lowering drug
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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Liu, H.-T.; He, H.-W.; Bai, X.-G.; Wang, J.-X.; Xu, C.-L.; Cai, S.-Y.; Shao, R.-G.; Wang, Y.-C. Arylsulfonylamino-Benzanilides as Inhibitors of the Apical Sodium-Dependent Bile Salt Transporter (SLC10A2). Molecules 2013, 18, 6883-6897.

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