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Master Thesis

Promédicaments à fonction carbamate : description du concept et application à la synthèse de molécules d’intérêt dans le traitement de la maladie d’Alzheimer

Abstract : Described in 1959, prodrugs have existed since the end of the 19th century. These drugs allow to modify the pharmacokinetic properties of an active substance. Some are composed of a carbamate function which, among other things, and which are hydrolyzed in the presence cholinesterases. These latter enzymes are a prime target in Alzheimer's disease (AD). Currently, no curative treatment exists to treat AD. ChE could also serve as an activating protein for pleiotropic prodrugs. Indeed, inhibiting central ChE with brain-penetrating designed carbamates which are able to covalently bind to the enzyme and to concomitantly liberate active metabolites in the brain could constitute a clinically more efficient approach which, additionally, is less likely to cause peripheral side effects. This thesis allowed to perform a digest state of the art of prodrugs composed of a carbamate group and opened up new synthetic pathways, coupled with in vitro and in vivo studies of pleiotropic prodrugs targeting both ChE with second therapeutic target. This polyactivity could provide patients with AD with real therapeutic benefits, both symptomatic and curative, as well as relative safety.
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Master Thesis
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https://dumas.ccsd.cnrs.fr/dumas-03078422
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Submitted on : Wednesday, December 16, 2020 - 4:47:24 PM
Last modification on : Tuesday, October 19, 2021 - 11:34:51 PM
Long-term archiving on: : Wednesday, March 17, 2021 - 7:47:02 PM

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  • HAL Id : dumas-03078422, version 1

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François-Xavier Toublet. Promédicaments à fonction carbamate : description du concept et application à la synthèse de molécules d’intérêt dans le traitement de la maladie d’Alzheimer. Sciences pharmaceutiques. 2020. ⟨dumas-03078422⟩

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