Design, synthesis and activity of ascorbic acid prodrugs of nipecotic, kynurenic and diclophenamic acids, liable to increase neurotropic activity

Stefano Manfredini, Barbara Pavan, Silvia Vertuani, Martina Scaglianti, Donatello Compagnone, Carla Biondi, Angelo Scatturin, Sergio Tanganelli, Luca Ferraro, Puttur Prasad, Alessandro Dalpiaz

Research output: Contribution to journalArticlepeer-review

85 Scopus citations

Abstract

To improve the entry of certain drugs into brain, ascorbic acid (AA) conjugates of these drugs were synthesized and their capacity to interact with SVCT2 ascorbate transporters was explored. Kinetic studies clearly indicate that all of the conjugates were able to competitively inhibit ascorbate transport in human retinal pigment epithelial cells (HRPE). In vivo studies, in a mouse model system, demonstrate that conjugate 3 is better absorbed compared to the nonconjugated parent drug.

Original languageEnglish (US)
Pages (from-to)559-562
Number of pages4
JournalJournal of Medicinal Chemistry
Volume45
Issue number3
DOIs
StatePublished - Jan 31 2002

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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