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Bioorg Med Chem Lett. 2007 Jan 15;17(2):444-7. Epub 2006 Oct 17.

Design and synthesis of substrate-mimic inhibitors of mycothiol-S-conjugate amidase from Mycobacterium tuberculosis.

Author information

1
Laboratory of Bioorganic Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892, USA.

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.

PMID:
17084627
DOI:
10.1016/j.bmcl.2006.10.031
[Indexed for MEDLINE]

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