increasing polarity in tacrine and huprine derivatives: potent anticholinesterase agents for the treatment of myasthenia gravis
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ID: 242564
2018
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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.
| Reference Key |
galdeano2018moleculesincreasing
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|---|---|
| Authors | ;Carles Galdeano;Nicolas Coquelle;Monika Cieslikiewicz-Bouet;Manuela Bartolini;Belén Pérez;M. Victòria Clos;Israel Silman;Ludovic Jean;Jacques-Philippe Colletier;Pierre-Yves Renard;Diego Muñoz-Torrero |
| Journal | Journal of ethnopharmacology |
| Year | 2018 |
| DOI |
10.3390/molecules23030634
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| URL | |
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