Current Topics in Medicinal Chemistry

Author(s): Pedro Merino, Mattia Ghirardello, Tomas Tejero, Ignacio Delso and Rosa Matute

DOI: 10.2174/1568026614666140423095331

Recent Advances on the Enantioselective Synthesis of C-Nucleosides Inhibitors of Inosine Monophosphate Dehydrogenase (IMPDH)

Page: [1212 - 1224] Pages: 13

  • * (Excluding Mailing and Handling)

Abstract

This review will describe the recent advances in the synthesis of C-nucleosides with inhibitory activity of inosine monophosphate dehydrogenase (IMPDH), a key enzyme in the biosynthesis of guanine nucleotides. The review will cover synthetic approaches of structural analogues showing modifications in the furanose ring as well as in the heterocyclic base. Heterocyclic sugar nucleoside analogues in which the furanose ring has been replaced by a different heterocyclic ring including aza analogues, thioanalogues as well as dioxolanyl and isoxazolidinyl analogues are also considered.

Keywords: C-Nucleosides, enzyme inhibitors, heterocyclic nucleosides, IMPDH, thiazole, tiazofurin.

Graphical Abstract