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Isoxazolotacrines as non-toxic and selective butyrylcholinesterase inhibitors for Alzheimer's disease

AuthorsCherif, O.; Allouche, F.; Chabchoub, Fakher; Chioua, Mourad ; Soriano, Elena ; Yáñez, Matilde; Cacabelos, Ramón; Romero, A. ; López, M. G.; Marco-Contelles, José
Issue Date2015
PublisherFuture Science
CitationFuture Medicinal Chemistry 6: 1883-1891 (2015)
AbstractBackground: Owing to the complex nature of Alzheimer's disease, there is a renewed and growing search for multitarget non-toxic tacrines as simple, easily available drugs in order to stop the progress and development of the disease. Results: This paper describes our preliminary results on the synthesis, in vitro biochemical evaluation and molecular modeling of isoxazolotacrines as potential drugs for the treatment of Alzheimer's disease. Novel 3-phenyl-5,6,7,8-tetrahydroisoxazolo[5,4-b]quinolin-4-amine (OC41) is a promising, 31% less toxic than tacrine in HepG2 cells, and selective reversible human butyrylcholinesterase inhibitor (IC50 = 5.08 ± 1.12 μM), also showing good drug-like properties according to the absorption, Distribution, Metabolism, Excretion, Toxicity analysis. Conclusion: A new family of non-hepatotoxic permeable tacrine analogs, showing selective butyrylcholinesterase inhibition, have been discovered for the potential treatment of Alzheimer's disease.
Identifiersdoi: 10.4155/fmc.14.115
issn: 1756-8919
e-issn: 1756-8927
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