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NUCLEOSIDE PRODRUGS OF A3 ADENOSINE RECEPTOR AGONISTS AND ANTAGONISTS.

Pedro Besada1, Liaman K Mamedova1, Krishnan K Palaniappan1

  • 1Molecular Recognition Section, Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892-0810, U.S.A.

Collection of Czechoslovak Chemical Communications
|November 24, 2021
PubMed
Summary

Researchers developed prodrugs of A3 adenosine receptor (AR) agonists and antagonists for in vivo delivery. These prodrugs showed reduced activity but were effectively hydrolyzed in human blood, regenerating the parent compounds for potential in vivo applications.

Keywords:
Adenosine receptorsAdenylate cyclaseG protein-coupled receptorsNucleosidesProdrugsPurinesReceptor binding assays

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Area of Science:

  • Medicinal Chemistry
  • Pharmacology
  • Nucleoside Chemistry

Background:

  • Selective agonists and antagonists of the A3 adenosine receptor (AR) are valuable therapeutic agents.
  • Direct in vivo delivery of these compounds can be challenging.
  • Prodrug strategies are employed to improve drug delivery and pharmacokinetic profiles.

Purpose of the Study:

  • To derivatize A3AR selective agonists and antagonists into prodrugs for in vivo delivery.
  • To evaluate the activity and in vivo stability of these novel prodrug derivatives.

Main Methods:

  • Acylation of free hydroxy groups at the 2' and 3' positions of A3AR ligands.
  • Radioligand binding assays and adenylate cyclase functional assays to assess activity.
  • Hydrolysis studies in human blood to determine prodrug cleavage rates.

Main Results:

  • Prodrug derivatives exhibited significantly lower activity compared to parent compounds in binding and functional assays.
  • Nucleoside 2',3'-diester prodrugs were successfully hydrolyzed in human blood, regenerating the parent A3AR agonists and antagonists.
  • Cleavage rates varied with ester chain length, with dipropionate esters being rapidly cleaved within two hours.

Conclusions:

  • Acylated prodrugs serve as effective masked forms of A3AR agonists and antagonists.
  • Demonstrated in vitro hydrolysis in human blood supports the potential for in vivo activation.
  • These prodrugs are suitable for future in vivo evaluation for therapeutic applications targeting the A3AR.