Synthesis and evaluation of NHC derivatives and 4′-fluorouridine prodrugs
Li Xiang, Tianwen Hu, Haitao Xue, Wenfang Pan, Yuanchao Xie, Jingshan Shen
Abstract
. The NHC derivatives were found inactive, but 4'-fluorouridine and its prodrugs had potent anti-RSV and anti-IFV activities. 4'-Fluorouridine was proved to be a nucleoside with poor stability, but the tri-ester prodrugs exhibited enhanced stability, especially tri-isobutyrate ester 1a. This prodrug also showed excellent oral pharmacokinetic properties in rats, with potential to be an oral antiviral candidate.
Topics & Concepts
ProdrugChemistryCombinatorial chemistryStereochemistryBiochemistryRespiratory viral infections researchPneumocystis jirovecii pneumonia detection and treatmentN-Heterocyclic Carbenes in Organic and Inorganic Chemistry