Parceria: Sabrina Baptista Ferreira - LaSOPB – Laboratório de Síntese Orgânica e Prospecção Biológica, Instituto de Química, Universidade Federal do Rio de Janeiro, Rio de Janeiro, RJ, 21941-909, Brazil
Emil Lindäckb e Magne O. Sydnesb - Department of Chemistry, Bioscience and Environmental Engineering, Faculty of Science and Technology, University of Stavanger, 4036, Stavanger, Norway
Óscar López - Departamento de Química Orgánica, Facultad de Química, Universidad de Sevilla, c/Profesor García González 1, 41012 Seville, Spain
Projeto: Alzheimer’s disease, which affects millions of people around the globe, is a fatal neurodegenerative disorder that affects the central nerve system with only 5 approved drugs used for the treatment. For this reason, it is necessary to develop new compounds that can be used as pharmaceuticals against the disease. Out of those five, the mode of action for three of them is to inhibit acetylcholinesterase (AChE) and by such means increase the levels of acetylcholine in the brain. In this context, we addressed two new classes of compounds based on iminosugars as dual-binding acetylcholinesterase inhibitors binding to two sites of acetylcholinesterase simultaneously. Two groups of compounds were synthesized, isofagomine-coumarin and deoxynojirimycin-benzotriazole heterodimers in yields ranging from 25-44% and 48-70% respectively. Currently, compounds are being screened for their biological activity as AChE inhibitors in Spain. Therefore, the project still progressing and once the biological testing is finished it will allow the publication of the work in at least 2 papers. Since the COVID outbreak started, all scientific conferences were cancelled in Norway and around Europe. However, the department where I was located at the University of Stavanger promoted regular meetings and discussions, allowing all researches to interact and build connections with each other. Looking into the future, we have been building a strong collaboration with Professor Sydnes at University of Stavanger. We already published two articles together in the past year and have others to come from my time there in 2020.
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