Design and synthesis of novel chalcones as potent selective monoamine oxidase-B inhibitors
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- 作者：Arwa Hammudaa ; Raed Shalabya ; Stefano Rovidab ; Dale E. Edmondsonc ; Claudia Bindab ; Ashraf Khalila ; akhalil@qu.edu.qa" class="auth_mail" title="E-mail the corresponding author
- 关键词：Monoamine oxidase ; Neuroprotection ; Drug design ; Synthesis ; Enzyme ; Chalcones
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：23 May 2016
- 年：2016
- 卷：114
- 期：Complete
- 页码：162-169
- 全文大小：1352 K
文摘
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Novel chalcone analogs were designed and synthesized as human MAO-B reversible inhibitors.
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The inhibitors bind with micromolar to submicromolar potency.
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The molecular scaffold determines high MAO-A/MAO-B selectivity.
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A double conformation in MAO-B active site is predicted by molecular docking.