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Aryl Guanyl Hydrazones: A Viable Strategy for Designing BBB-Permeable, Neuroactive Compounds?

Eleonora Colombo1,2, Leonardo Maiorana1, Greta Donati3

  • 1Chemistry Department, Università degli Studi di Milano, Via Golgi 19, 20133 Milan, Italy.

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Summary

Aryl guanyl hydrazones offer tunable properties for drug discovery, enhancing blood-brain barrier permeability due to their lipophilicity at physiological pH. Their adaptable charge distribution aids in binding to diverse biological targets.

Keywords:
BBBNMRaryl guanyl hydrazonesbioavailabilitynucleic acid bindingpKarational drug designtautomeric equilibria

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Area of Science:

  • Medicinal Chemistry
  • Organic Chemistry
  • Pharmacology

Background:

  • Guanyl hydrazones are versatile functional groups with tunable properties.
  • Aryl guanyl hydrazones possess lower pKa values than aliphatic counterparts, promoting ionization at physiological pH.
  • This ionization state increases lipophilicity and blood-brain barrier (BBB) permeability.

Purpose of the Study:

  • To review (hetero)aromatic drugs, clinical candidates, leads, and hits containing guanyl hydrazone moieties.
  • To discuss their mechanisms of action, in vitro, and in vivo potency.
  • To explore synthetic routes and future trends for aryl guanyl hydrazones in CNS and PNS drug discovery.

Main Methods:

  • Literature review of existing drugs and drug candidates.
  • Analysis of structure-activity relationships related to guanyl hydrazone functional groups.
  • Brief presentation of synthetic methodologies for guanyl hydrazone synthesis.

Main Results:

  • Aryl guanyl hydrazones demonstrate significant potential in drug discovery due to their favorable physicochemical properties.
  • Their tautomeric equilibria allow for flexible charge allocation, enhancing binding to protein and nucleic acid targets.
  • Examples of successful drug candidates incorporating these moieties were identified.

Conclusions:

  • Aryl guanyl hydrazones are promising scaffolds for developing novel therapeutics, particularly for central nervous system (CNS) and peripheral nervous system (PNS) disorders.
  • Their unique properties facilitate improved drug delivery and target engagement.
  • Further research into synthetic strategies and biological applications is warranted.