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Increasing Polarity in Tacrine and Huprine Derivatives: Potent Anticholinesterase Agents for the Treatment of Myasthenia Gravis.
Polarité croissante dans les dérivés de la tacrine et de l'huprine: puissants agents anticholinestérasiques pour le traitement de la myasthénie grave.
Galdeano C 1 , Coquelle N 2, 3 , Cieslikiewicz-Bouet M 4 , Bartolini M 5 , Pérez B 6 , Clos MV 7 , Silman I 8 , Jean L 9 , Colletier JP 10 , Renard PY 11 , Muñoz-Torrero D 12 .
Molécules. 2018 mars 11; 23 (3). pii: E634. doi: 10,3390 / molécules23030634.
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.
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