Arylsulfonylamino-benzanilides as inhibitors of the apical sodium-dependent bile salt transporter (SLC10A2)

Molecules. 2013 Jun 10;18(6):6883-97. doi: 10.3390/molecules18066883.

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anilides / chemical synthesis
  • Anilides / chemistry*
  • Anilides / pharmacology*
  • Arylsulfonates / chemistry*
  • Cell Line
  • Drug Design
  • Humans
  • Molecular Structure
  • Organic Anion Transporters, Sodium-Dependent / antagonists & inhibitors*
  • Symporters / antagonists & inhibitors*

Substances

  • Anilides
  • Arylsulfonates
  • Organic Anion Transporters, Sodium-Dependent
  • Symporters
  • sodium-bile acid cotransporter
  • benzanilide