Synthesis and Evaluation of 2-Azetidinone and 1H-Pyrrole-2,5-dione Derivatives as Cholesterol Absorption Inhibitors for Reducing Inflammation Response and Oxidative Stress

Article abstract of DOI:10.1002/cbdv.201800189

Excess lipid accumulation can initiate the development and progression of atherosclerotic lesions, thus eventually leading to cardiovascular disease. Lipid-lowering medication therapy is one of the cornerstones of cardiovascular disease therapy. On the basis of the cholesterol absorption inhibitor ezetimibe, we successfully synthesized seven 2-azetidinone derivatives and eighteen 1H-pyrrole-2,5-dione derivatives. Most of the new compounds significantly inhibited cholesterol uptake in vitro. In addition, one of the most active inhibitors, 3-(4-fluorophenyl)-1-[(3S)-3-hydroxy-3-(4-hydroxyphenyl)propyl]-4-(4-hydroxyphenyl)-1H-pyrrole-2,5-dione (14q), showed no cytotoxicity in L02 and HEK293T cell lines. Further evaluation indicated that 14q inhibited considerably the amount of TNF-α, ROS, MDA, and LDH in vitro. Therefore, 14q might be a novel cholesterol absorption inhibitor.

Full text of DOI:10.1002/cbdv.201800189

Title: Synthesis and evaluation of 2-azetidinone and 1H-pyrrole-2,5-
dione derivatives as cholesterol absorption inhibitors for reducing
inflammation response and oxidative stress
Authors: Yineng Xia, Lijuan Zhu, Xinrui Yuan, and Yubin Wang
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To be cited as: Chem. Biodiversity 10.1002/cbdv.201800189
Link to VoR: http://dx.doi.org/10.1002/cbdv.201800189

10.1002/cbdv.201800189
Chemistry & Biodiversity
Chem. Biodiversity
This article is protected by copyright. All rights reserved.

10.1002/cbdv.201800189
Chemistry & Biodiversity
Chem. Biodiversity
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10.1002/cbdv.201800189
Chemistry & Biodiversity
Chem. Biodiversity
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This article is protected by copyright. All rights reserved.

10.1002/cbdv.201800189
Chemistry & Biodiversity
Chem. Biodiversity
This article is protected by copyright. All rights reserved.

10.1002/cbdv.201800189
Chemistry & Biodiversity
Chem. Biodiversity
This article is protected by copyright. All rights reserved.

10.1002/cbdv.201800189
Chemistry & Biodiversity
Chem. Biodiversity
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This article is protected by copyright. All rights reserved.

10.1002/cbdv.201800189
Chemistry & Biodiversity
Chem. Biodiversity
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This article is protected by copyright. All rights reserved.

10.1002/cbdv.201800189
Chemistry & Biodiversity
Chem. Biodiversity
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This article is protected by copyright. All rights reserved.

10.1002/cbdv.201800189
Chemistry & Biodiversity
Chem. Biodiversity
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This article is protected by copyright. All rights reserved.

10.1002/cbdv.201800189
Chemistry & Biodiversity
Chem. Biodiversity
This article is protected by copyright. All rights reserved.