Memantine prodrug as a new agent for Alzheimer's Disease.

ABSTRACT: Hydrogen sulphide has recently drawn much attention due to its potent anti-inflammatory and neuroprotective roles in brain functions. The purpose of the current study was to exploit these beneficial properties of H₂S to design a new agent for the treatment of Alzheimer's disease (AD). To pursue our aims, we replaced the free amine group of memantine with an isothiocyanate functionality as a putative H₂S-donor moiety. The new chemical entity, named memit, was then tested in vitro to determine whether it retains the pharmacological profile of the "native drug", while also providing a source of H₂S in the CNS. Indeed, Memit showed the ability to release H₂S through a cysteine-mediated mechanism, thus generating memantine. Moreover, the new hybrid mo

SUBMITTER: Sestito S 

PROVIDER: S-EPMC6420495 | biostudies-literature | 2019 Mar

REPOSITORIES: biostudies-literature