Synthesis and Biological Evaluation of Ezetimibe Analogs as Possible Cholesterol Absorption Inhibitors

In order to investigate the SAR of Ezetimibe analogs for cholesterol absorption inhibitions, amide group and electron-deficient pyridine ring were introduced to the C-(3) carbon chain of Ezetimibe. Eight new derivatives of the 2-azetidinone cholesterol absorption inhibitors have been synthesized, an...

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Detalles Bibliográficos
Autores principales: Wang, Yubin, Haiqian, Huang, Wenlong, Zhang, Huibin, Zhou, Jinpei
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Bentham Science Publishers Ltd 2011
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3179128/
https://www.ncbi.nlm.nih.gov/pubmed/21966284
http://dx.doi.org/10.2174/157018011795906776
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author Wang, Yubin
Haiqian,
Huang, Wenlong
Zhang, Huibin
Zhou, Jinpei
author_facet Wang, Yubin
Haiqian,
Huang, Wenlong
Zhang, Huibin
Zhou, Jinpei
author_sort Wang, Yubin
collection PubMed
description In order to investigate the SAR of Ezetimibe analogs for cholesterol absorption inhibitions, amide group and electron-deficient pyridine ring were introduced to the C-(3) carbon chain of Ezetimibe. Eight new derivatives of the 2-azetidinone cholesterol absorption inhibitors have been synthesized, and all of them were enantiomerically pure. All the new compounds were evaluated for their activity to inhibit cholesterol absorption in hamsters, and most of them showed comparable effects in lowering the levels of total cholesterol in the serum.
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spelling pubmed-31791282011-09-30 Synthesis and Biological Evaluation of Ezetimibe Analogs as Possible Cholesterol Absorption Inhibitors Wang, Yubin Haiqian, Huang, Wenlong Zhang, Huibin Zhou, Jinpei Lett Drug Des Discov Article In order to investigate the SAR of Ezetimibe analogs for cholesterol absorption inhibitions, amide group and electron-deficient pyridine ring were introduced to the C-(3) carbon chain of Ezetimibe. Eight new derivatives of the 2-azetidinone cholesterol absorption inhibitors have been synthesized, and all of them were enantiomerically pure. All the new compounds were evaluated for their activity to inhibit cholesterol absorption in hamsters, and most of them showed comparable effects in lowering the levels of total cholesterol in the serum. Bentham Science Publishers Ltd 2011-07 /pmc/articles/PMC3179128/ /pubmed/21966284 http://dx.doi.org/10.2174/157018011795906776 Text en © 2011 Bentham Science Publishers Ltd. http://creativecommons.org/licenses/by/2.5/ This is an open access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/2.5/), which permits unrestrictive use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Article
Wang, Yubin
Haiqian,
Huang, Wenlong
Zhang, Huibin
Zhou, Jinpei
Synthesis and Biological Evaluation of Ezetimibe Analogs as Possible Cholesterol Absorption Inhibitors
title Synthesis and Biological Evaluation of Ezetimibe Analogs as Possible Cholesterol Absorption Inhibitors
title_full Synthesis and Biological Evaluation of Ezetimibe Analogs as Possible Cholesterol Absorption Inhibitors
title_fullStr Synthesis and Biological Evaluation of Ezetimibe Analogs as Possible Cholesterol Absorption Inhibitors
title_full_unstemmed Synthesis and Biological Evaluation of Ezetimibe Analogs as Possible Cholesterol Absorption Inhibitors
title_short Synthesis and Biological Evaluation of Ezetimibe Analogs as Possible Cholesterol Absorption Inhibitors
title_sort synthesis and biological evaluation of ezetimibe analogs as possible cholesterol absorption inhibitors
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3179128/
https://www.ncbi.nlm.nih.gov/pubmed/21966284
http://dx.doi.org/10.2174/157018011795906776
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AT zhanghuibin synthesisandbiologicalevaluationofezetimibeanalogsaspossiblecholesterolabsorptioninhibitors
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