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Dihydroquinoline Carbamate Derivatives as "Bio-oxidizable" Prodrugs for Brain Delivery of Acetylcholinesterase Inhibitors: [¹¹C] Radiosynthesis and Biological Evaluation

Archive ouverte | Bohn, Pierre | CCSD

LDM TEP COLL. International audience. With the aim of improving the efficiency of marketed acetylcholinesterase (AChE) inhibitors in the symptomatic treatment of Alzheimer’s disease, plagued by adverse effects arisi...

Solid phase synthesis of a redox delivery system with the aim of targeting peptides into the brain.

Archive ouverte | Patteux, Claudine | CCSD

International audience. A solid phase approach for the preparation of peptides attached to a redox chemical delivery system derived from stable annulated NADH models is reported. The synthesis starts with the grafti...

Dihydroquinoline Carbamate DQS1-02 as a Prodrug of a Potent Acetylcholinesterase Inhibitor for Alzheimer’s Disease Therapy: Multigram-Scale Synthesis, Mechanism Investigations, in Vitro Safety Pharmacology, and Preliminary in Vivo Toxicology Profile

Archive ouverte | Alix, Florent | CCSD

International audience. We previously characterized a set of potent pseudo-irreversible inhibitors of acetylcholinesterase (AChE) based on a redox prodrug strategy. Among the various synthesized prodrugs, compound 1...

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