Arylpiperidines as a new class of oxidosqualene cyclase inhibitors
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- 作者：Marco Kellera ; Annette Wolfgardta ; Christoph Mü ; llera ; Rainer Wilckenb ; Frank M. Bö ; cklerb ; Simonetta Oliaro-Bossoc ; Terenzio Ferrantec ; Gianni Ballianoc ; Franz Brachera ; Franz.Bracher@cup.uni-muenchen.de" class="auth_mail" title="E-mail the corresponding author
- 关键词：Oxidosqualene cyclase ; Enzyme inhibitor ; High energy intermediate ; Arylpiperidine ; Docking experiments
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：15 February 2016
- 年：2016
- 卷：109
- 期：Complete
- 页码：13-22
- 全文大小：1020 K
文摘
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Arylpiperidines are a new class of oxidosqualene cyclase inhibitors.
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They are steroidomimetic compounds mimicking cationic high energy intermediates.
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Compound 29 has submicromolar activity on human OSC and high species selectivity.
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This compound effectively reduces total cholesterol biosynthesis in a cellular assay.
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A plausible binding mode is suggested on the basis of docking experiments.