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dc.contributor.authorCherif, O.-
dc.contributor.authorAllouche, F.-
dc.contributor.authorChabchoub, Fakher-
dc.contributor.authorChioua, Mourad-
dc.contributor.authorSoriano, Elena-
dc.contributor.authorYáñez, Matilde-
dc.contributor.authorCacabelos, Ramón-
dc.contributor.authorRomero, A.-
dc.contributor.authorLópez, M. G.-
dc.contributor.authorMarco-Contelles, José-
dc.identifierdoi: 10.4155/fmc.14.115-
dc.identifierissn: 1756-8919-
dc.identifiere-issn: 1756-8927-
dc.identifier.citationFuture Medicinal Chemistry 6: 1883-1891 (2015)-
dc.description.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.-
dc.publisherFuture Science-
dc.titleIsoxazolotacrines as non-toxic and selective butyrylcholinesterase inhibitors for Alzheimer's disease-
dc.description.versionPeer Reviewed-
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