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Oxidation-reduction or redox reactions involve the transfer of electrons from one molecule or atom to another. When an atom gains an electron, another atom must lose an electron, meaning oxidation and reduction must occur together. Since the redox occurs in pairs, the atom that gets oxidized is also called the reducing agent or reductant, and the atom that is reduced is also called the oxidizing agent or oxidant. A straightforward way to remember the definitions of oxidation and reduction is...

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Chemogenetic Regulation in Reprogrammed Stem Cell-derived Precursor Cells in Treating Neurodegenerative Diseases

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Redox Heterocyclic Platforms Engineered for Brain Drug Delivery and Beyond.

Cyril Papamicaël¹, Vincent Gembus¹, Fabienne Gourand²

¹CNRS, INSA Rouen Normandie, Univ Rouen Normandie, Univ Caen Normandie, ENSICAEN, Institut CARMeN UMR6064, Rouen, France.

Chemical Record (New York, N.Y.)

|May 28, 2026

Summary

Researchers developed redox-responsive heterocycles, like 1,4-dihydroquinolines, for targeted brain drug delivery. These novel prodrugs enhance transport for central nervous system disorders and imaging.

Keywords:

blood–brain barrier brain drug delivery dihydropyridine dihydroquinoline redox‐responsive prodrugs

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Area of Science:

Medicinal Chemistry
Neuroscience
Organic Synthesis

Background:

The blood-brain barrier (BBB) presents a significant obstacle for treating central nervous system (CNS) disorders.
Effective drug delivery to the brain is crucial for diagnosing and treating neurological conditions.
Prodrug strategies are vital for enhancing drug permeability across biological barriers.

Purpose of the Study:

To present contributions to redox-responsive heterocycles for targeted brain delivery.
To showcase the development of novel prodrugs based on 1,4-dihydroquinolines and 1,4-dihydropyridines.
To explore applications in CNS disease treatment and brain imaging.

Main Methods:

Utilizing chemical delivery system and bioprecursor prodrug strategies.
Designing redox-activated drug carriers and "bio-oxidizable" prodrugs.
Investigating applications for neurotransmitters, neuropeptides, radiotracers, and enzyme inhibitors.

Main Results:

Demonstrated efficient transport of various molecules across the BBB.
Developed prodrugs for potential Alzheimer's disease therapeutics (cholinesterase and kinase inhibitors).
Enabled advanced brain imaging through targeted radiotracer delivery.

Conclusions:

Redox-responsive heterocycles offer a versatile platform for overcoming the BBB.
These systems facilitate targeted delivery for both therapeutic and diagnostic CNS applications.
The heterocyclic systems also advance synthetic methodologies in peptide synthesis and amide bond formation.