Synthesis of Monomeric Derivatives To Probe Memoquin鈥檚 Bivalent Interactions

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• 作者：Maria Laura Bolognesi ; GianPaolo Chiriano ; Manuela Bartolini ; Francesca Mancini ; Giovanni Bottegoni ; Valentina Maestri ; Stefan Czvitkovich ; Manfred Windisch ; Andrea Cavalli ; Anna Minarini ; Michela Rosini ; Vincenzo Tumiatti ; Vincenza Andrisano ; Carlo Melchiorre
• 刊名：Journal of Medicinal Chemistry
• 出版年：2011
• 出版时间：December 22, 2011
• 年：2011
• 卷：54
• 期：24
• 页码：8299-8304
• 全文大小：391K
• 年卷期：v.54,no.24(December 22, 2011)
• ISSN：1520-4804

文摘

Eight monomeric congeners, related to the multitarget lead candidate memoquin, were prepared and evaluated at multiple targets to determine their profile against Alzheimer鈥檚 disease. 2鈥?b>4 bind to AChE with similar low nanomolar affinities and function as effective inhibitors of amyloid aggregation. The most potent monovalent ligand 2 also inhibits BACE-1 in vitro and APP metabolism in primary chicken telencephalic neurons.