Current Topics in Medicinal Chemistry

Allen B. Reitz
Fox Chase Chemical Diversity Center, Inc.
Doylestown, PA


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

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

Affiliation: Laboratorio de Sintesis Asimetrica. Departamento de Sintesis y Estructura de Biomoleculas. ISQCH. Universidad de Zaragoza. CSIC. Campus San Francisco. Zaragoza, Aragon, Spain.

Graphical 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 Heterocyclic sugar nucleoside analogues in which the furanose ring has been replaced by a different heterocyclic ring including aza analogues, thioanalogues as well as dioxolanyl and isoxazolidinyl analogues are also considered.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.

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Article Details

Page: [1212 - 1224]
Pages: 13
DOI: 10.2174/1568026614666140423095331