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  • Title: Design and synthesis of substrate-mimic inhibitors of mycothiol-S-conjugate amidase from Mycobacterium tuberculosis.
    Author: Metaferia BB, Ray S, Smith JA, Bewley CA.
    Journal: Bioorg Med Chem Lett; 2007 Jan 15; 17(2):444-7. PubMed ID: 17084627.
    Abstract:
    The Staudinger reaction between a polymer-supported triphenylphosphine reagent and pseudo-disaccharide azides is successfully applied to synthesize a variety of substrate-mimic mycothiol analogs. Screening of this new group of analogs against the mycobacterial detoxification enzyme mycothiol-S-conjugate amidase (MCA) yielded several modest inhibitors (IC50 values around 50 microM) and provided additional structure-activity relationships for future optimization of inhibitors of MCA and its homologs.
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