Novel series of tacrine-tianeptine hybrids: Synthesis, cholinesterase inhibitory activity, S100B secretion and a molecular modeling approach
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- 作者：Marco Antonio Ceschia ; mceschi@iq.ufrgs.br" class="auth_mail" title="E-mail the corresponding author ; Jessie Sobieski da Costaa ; Joã ; o Paulo Bizarro Lopesa ; Viktor Saraiva Câ ; maraa ; Leandra Franciscato Campoa ; Antonio Cé ; sar de Amorim Borgesa ; Carlos Alberto Saraiva Gonç ; alvesb ; Daniela Fraga de Souzab ; Eduardo Luis Konrathc ; Ana Luiza Martins Karld ; Isabella Alvim Guedesd ; Laurent Emmanuel Dardenned ; dardenne@lncc.br" class="auth_mail" title="E-mail the corresponding author
- 关键词：Tacrine ; Tianeptine ; AChE ; BuChE ; S100B secretion ; Coupling reaction ; Molecular modeling
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：4 October 2016
- 年：2016
- 卷：121
- 期：Complete
- 页码：758-772
- 全文大小：2922 K
文摘
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New tacrine-tianeptine hybrids were synthesized.
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AChE and BuChE inhibitory activities were performed.
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Molecular modeling studies using the X-ray structure of TcAChE.
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Two compounds were able to reduce the in vitro basal secretion of S100B.