Novel glycosyl prodrug of RXP03 as MMP-11 prodrug: design, synthesis and virtual screening

Moaz M. Abdou*, Ferenc Ötvös, Dewen Dong, Magdalini Matziari

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

Abstract

Like most phosphinic acids, the potent and selective RXP03 inhibitor of different MMPs exhibited moderate absorption and low bioavailability, which impaired its use. In an unprecedented attempt, we present an interesting synthetic approach to a new class of phosphinate prodrug, glycosyl ester of RXP03, to provide a potentially improved blood–brain barrier (BBB) behavior compared to the former lead compound RXP03. To validate this speculation, a predictive study for permeability enhancer of glycosyl ester of RXP03 showed encouraging insights to improve drug delivery across biological barriers.

Original languageEnglish
Article number167
JournalBMC Chemistry
Volume17
Issue number1
DOIs
Publication statusPublished - Dec 2023

Keywords

  • Matrix metalloproteases
  • Molecular docking
  • Permeability enhancer
  • Phosphinic ester
  • Prodrug
  • RXP03

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