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Showing 1–13 of 13 results
Advanced filters: Author: Michael Meanwell Clear advanced filters

  • C4ʹ-modified nucleoside analogues attract global attention, but current approaches for the synthesis involve lengthy, nonmodular routes. Herein, the authors report a modular 5-step process to a diverse collection of C4ʹ-modified nucleoside analogues through a sequence of intramolecular trans-acetalizations of polyhydroxylated frameworks.

    • Thirupathi Nuligonda
    • Gautam Kumar
    • Michael W. Meanwell
    ResearchOpen Access
    Nature Communications
    Volume: 15, P: 1-7

  • The metal cations released from sacrificial anodes during reductive electrosynthetic reactions are widely believed to not affect reaction outcomes. Here, the authors disclose an electrochemical deutero-(di)carboxylation that relies on anodically generated Mg2+ cations to achieve selectivity in both the site and amount of deuteration.

    • Subhojit Mondal
    • Sahil
    • Michael W. Meanwell
    ResearchOpen Access
    Nature Communications
    Volume: 16, P: 1-10

  • Iminosugars are biologically and medicinally important compounds but methods for their synthesis are often laborious. Here, the authors report a simple, rapid route for the enantioselective synthesis of multiple biologically active iminosugars and C-nucleoside analogues.

    • Milan Bergeron-Brlek
    • Michael Meanwell
    • Robert Britton
    ResearchOpen Access
    Nature Communications
    Volume: 6, P: 1-6

  • Nucleoside diphosphates and triphosphates impact nearly every aspect of biochemistry. Now, a modular, reagent-based platform has been developed to enable the stereocontrolled and scalable synthesis of a library of such molecules. This operationally simple approach provides access to pure stereoisomers of nucleoside α-thiodiphosphates and α-thiotriphosphates.

    • Hai-Jun Zhang
    • Michał Ociepa
    • Phil S. Baran
    Research
    Nature Chemistry
    Volume: 16, P: 249-258

  • Mechanism-based inhibitors of glycoside hydrolases are useful probes for basic research and represent potential drug candidates. Here, the authors present a series of mechanism-based covalent α-galactosidase inhibitors and elucidate the kinetic and structural basis of their inhibitory activity.

    • Weiwu Ren
    • Robert Pengelly
    • Andrew J. Bennet
    ResearchOpen Access
    Nature Communications
    Volume: 9, P: 1-12

  • Almost 200 million people worldwide are chronically infected with hepatitis C virus. Current treatments are poorly tolerated and not wholly effective, so new drugs are needed. Here, a potent new inhibitor of hepatitis C virus is described. This inhibitor targets the viral protein NS5A, and shows potential as part of a therapeutic regimen based on a combination of viral inhibitors.

    • Min Gao
    • Richard E. Nettles
    • Lawrence G. Hamann
    Research
    Nature
    Volume: 465, P: 96-100

  • The development of nucleoside analogs for use as antiviral agents and antisense oligonucleotides requires efficient synthetic methods. This three-step approach starts with proline-catalyzed fluorination of simple heteroaryl-substituted aldehydes.

    • Emma K. Davison
    • David A. Petrone
    • Robert Britton
    Protocols
    Nature Protocols
    Volume: 17, P: 2008-2024

  • This Primer describes contemporary fluorination and fluoroalkylation reactions in chemical synthesis. The authors describe the main fluorination and fluoroalkylation reactions. The many applications of these reactions in pharmaceuticals, imaging agents and agriculture are discussed, along with the history and future of synthetic organofluorine chemistry.

    • Robert Britton
    • Veronique Gouverneur
    • Jinbo Hu
    Reviews
    Nature Reviews Methods Primers
    Volume: 1, P: 1-22

  • Prodrug strategies can be used to overcome pharmacokinetic and pharmacodynamic issues in many therapeutic agents. Here, Rautio and colleagues discuss which approaches have been most successful, particularly in the past 10 years, and highlight the challenges in incorporating prodrug moieties during drug development.

    • Jarkko Rautio
    • Nicholas A. Meanwell
    • Michael J. Hageman
    Reviews
    Nature Reviews Drug Discovery
    Volume: 17, P: 559-587

  • Glycomimetics are structural mimics of carbohydrates that can replicate their biological activity but have improved drug-like properties. Here, using proline-catalysed α-halogenation/aldol cascades, carbohydrate building blocks are readily assembled and then diversified into glycomimetics including imino- and carbasugars.

    • Michael Meanwell
    • Gaelen Fehr
    • Robert Britton
    ResearchOpen Access
    Communications Chemistry
    Volume: 4, P: 1-9