Synthesis, pharmacological assessment, molecular modeling and in silico studies of fused tricyclic coumarin derivatives as a new family of multifunctional anti-Alzheimer agents
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- 作者：Jeelan Basha Shaika ; Bhagath Kumar Palakab ; Mohan Penumalaa ; Kasi Viswanath Kotapatib ; Subba Rao Devinenic ; Siddhartha Eadlapallid ; M. Manidhar Darlac ; Dinakara Rao Ampasalab ; Ramakrishna Vadded ; G. Damu Amoorua ; agdamu01@gmail.com" class="auth_mail" title="E-mail the corresponding author
- 关键词：Alzheimer's disease ; Fused tricyclic coumarin ; Antioxidant ; Acetylcholinesterase ; Butyrylcholinesterase ; Neuroprotection ; Molecular modeling study ; ADMET
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：1 January 2016
- 年：2016
- 卷：107
- 期：Complete
- 页码：219-232
- 全文大小：2006 K
文摘
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A series of 7,8-fused tricyclic coumarin derivatives (6a–s) were synthesized.
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Compounds were evaluated for AChE, BuChE, ABTS inhibitory and neuroprotective activities.
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Most compounds had potent and selective anti AChE activity superior to galantamine.
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N-(3-bromobenzyl) derivative 6n had excellent anti-AChE and antioxidant profile.
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Kinetic and docking studies showed dual binding site ability of 6n to inhibit AChE.