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Title: Shogaol-huprine hybrids: Dual antioxidant and anticholinesterase agents with beta-amyloid and tau anti-aggregating properties
Author: Pérez-Areales, F. Javier
Di Pietro, Ornella
Espargaró Colomé, Alba
Vallverdú i Queralt, Anna
Galdeano Cantador, Carlos
Ragusa, Ilaria M.
Viayna, Elisabet
Guillou, Catherine
Clos Guillén, M. Victòria
Pérez Fernández, Belén
Sabaté Lagunas, Raimon
Lamuela Raventós, Rosa Ma.
Luque Garriga, F. Xavier
Muñoz-Torrero López-Ibarra, Diego
Keywords: Disseny de medicaments
Malaltia d'Alzheimer
Inhibidors enzimàtics
Drug design
Alzheimer's disease
Enzyme inhibitors
Issue Date: 1-Oct-2014
Publisher: Elsevier Ltd
Abstract: Multitarget compounds are increasingly being pursued for the effective treatment of complex diseases. Herein, we describe the design and synthesis of a novel class of shogaol<br>huprine hybrids, purported to hit several key targets involved in Alzheimer"s disease. The hybrids have been tested in vitro for their inhibitory activity against human acetylcholinesterase and butyrylcholinesterase and antioxidant activity (ABTS.+, DPPH and Folin-Ciocalteu assays), and in intact Escherichia coli cells for their Aβ42 and tau anti-aggregating activity. Also, their brain penetration has been assessed (PAMPA-BBB assay). Even though the hybrids are not as potent AChE inhibitors or antioxidant agents as the parent huprine Y and [4]-shogaol, respectively, they still exhibit very potent anticholinesterase and antioxidant activities and are much more potent Aβ42 and tau anti-aggregating agents than the parent compounds. Overall, the shogaol<br>huprine hybrids emerge as interesting brain permeable multitarget anti-Alzheimer leads.
Note: Versió postprint del document publicat a:
It is part of: Bioorganic & Medicinal Chemistry, 2014, vol. 22, num. 19, p. 5298-5307
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ISSN: 0968-0896
Appears in Collections:Articles publicats en revistes (Farmacologia, Toxicologia i Química Terapèutica)
Articles publicats en revistes (Institut de Nanociència i Nanotecnologia (IN2UB))
Articles publicats en revistes (Institut de Biomedicina (IBUB))
Articles publicats en revistes (Farmàcia, Tecnologia Farmacèutica i Fisicoquímica)

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