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 Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China 2 Department of Internal Medicine and Liver Center, School of Medicine, Yale University, New Haven, CT 06520, USA
* Authors to whom correspondence should be addressed.
Received: 2 May 2013; in revised form: 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

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MDPI and ACS Style

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.

AMA Style

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(6):6883-6897.

Chicago/Turabian Style

Liu, Hong-Tao; He, Hong-Wei; Bai, Xiao-Guang; Wang, Ju-Xian; Xu, Chang-Liang; Cai, Shi-Ying; Shao, Rong-Guang; Wang, Yu-Cheng. 2013. "Arylsulfonylamino-Benzanilides as Inhibitors of the Apical Sodium-Dependent Bile Salt Transporter (SLC10A2)." Molecules 18, no. 6: 6883-6897.

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