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DC Field | Value | Language |
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dc.contributor.author | Galdeano Cantador, Carlos | - |
dc.contributor.author | Coquelle, Nicolas | - |
dc.contributor.author | Cieslikiewicz-Bouet, Monika | - |
dc.contributor.author | Bartolini, Manuela | - |
dc.contributor.author | Pérez, Belén | - |
dc.contributor.author | Clos, Victòria | - |
dc.contributor.author | Silman, Israel | - |
dc.contributor.author | Jean, Ludovic | - |
dc.contributor.author | Colletier, Jacques-Philippe | - |
dc.contributor.author | Renard, Pierre-Yves | - |
dc.contributor.author | Muñoz-Torrero López-Ibarra, Diego | - |
dc.date.accessioned | 2018-05-11T11:32:14Z | - |
dc.date.available | 2018-05-11T11:32:14Z | - |
dc.date.issued | 2018-03-11 | - |
dc.identifier.issn | 1420-3049 | - |
dc.identifier.uri | http://hdl.handle.net/2445/122306 | - |
dc.description.abstract | Symptomatic treatment of myasthenia gravis is based on the use of peripherally-acting acetylcholinesterase (AChE) inhibitors that, in some cases, must be discontinued due to the occurrence of a number of side-effects. Thus, new AChE inhibitors are being developed and investigated for their potential use against this disease. Here, we have explored two alternative approaches to get access to peripherally-acting AChE inhibitors as new agents against myasthenia gravis, by structural modification of the brain permeable anti-Alzheimer AChE inhibitors tacrine, 6-chlorotacrine, and huprine Y. Both quaternization upon methylation of the quinoline nitrogen atom, and tethering of a triazole ring, with, in some cases, the additional incorporation of a polyphenol-like moiety, result in more polar compounds with higher inhibitory activity against human AChE (up to 190-fold) and butyrylcholinesterase (up to 40-fold) than pyridostigmine, the standard drug for symptomatic treatment of myasthenia gravis. The novel compounds are furthermore devoid of brain permeability, thereby emerging as interesting leads against myasthenia gravis. | - |
dc.format.extent | 19 p. | - |
dc.format.mimetype | application/pdf | - |
dc.language.iso | eng | - |
dc.publisher | MDPI | - |
dc.relation.isformatof | Reproducció del document publicat a: https://doi.org/10.3390/molecules23030634 | - |
dc.relation.ispartof | Molecules, 2018, vol. 23(3), num. 634 | - |
dc.relation.uri | https://doi.org/10.3390/molecules23030634 | - |
dc.rights | cc-by (c) Galdeano Cantador, Carlos et al., 2018 | - |
dc.rights.uri | http://creativecommons.org/licenses/by/3.0/es | - |
dc.source | Articles publicats en revistes (Farmacologia, Toxicologia i Química Terapèutica) | - |
dc.subject.classification | Acetilcolinesterasa | - |
dc.subject.classification | Triazoles | - |
dc.subject.classification | Malalties neuromusculars | - |
dc.subject.other | Acetylcholinesterase | - |
dc.subject.other | Triazoles | - |
dc.subject.other | Neuromuscular diseases | - |
dc.title | Increasing polarity in tacrine and huprine derivatives: Potent anticholinesterase agents for the treatment of myasthenia gravis | - |
dc.type | info:eu-repo/semantics/article | - |
dc.type | info:eu-repo/semantics/publishedVersion | - |
dc.identifier.idgrec | 679215 | - |
dc.date.updated | 2018-05-11T11:32:15Z | - |
dc.rights.accessRights | info:eu-repo/semantics/openAccess | - |
dc.identifier.pmid | 29534488 | - |
Appears in Collections: | Articles publicats en revistes (Institut de Biomedicina (IBUB)) Articles publicats en revistes (Farmacologia, Toxicologia i Química Terapèutica) |
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