Title of article
Design and synthesis of substrate-mimic inhibitors of mycothiol-S-conjugate amidase from Mycobacterium tuberculosis
Author/Authors
Belhu B. Metaferia، نويسنده , , Satyajit Ray، نويسنده , , Jeremy A. Smith، نويسنده , , Carole A. Bewley، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
4
From page
444
To page
447
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 μM) and provided additional structure–activity relationships for future optimization of inhibitors of MCA and its homologs.
Keywords
Mycothiol bimane , Quinic acid , Myo-d-inositol , Polymer-supported triphenyl phosphine , Pseudodisaccharide , mycobacteria
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2007
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
797672
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