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J Med Microbiol. 2006 Apr;55(Pt 4):407-15.

In vitro properties of antimicrobial bromotyrosine alkaloids.

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Division of Infectious Diseases, University of British Columbia, Vancouver, BC V5Z 3J5, Canada.


A bromotyrosine alkaloid family of antimicrobial agents was synthesized using the known structure of a natural inhibitor of the mycobacterial mycothiol S-conjugate amidase (MCA) as a template. This series of compounds represents a novel class of anti-infective agents against Gram-positive pathogens, including mycobacteria and meticillin- and vancomycin-resistant Staphylococcus aureus. The fact that these compounds are active against mycobacterial strains in which the MCA gene is deleted and against Gram-positive bacteria lacking mycothiol suggests the existence of an alternative target for these compounds. One member of this family, EXEG1706, was identified as the lead compound possessing low MICs (2.5-25 microg ml(-1)) for several clinical isolates, whilst having low toxicity for THP-1 monocytes and macrophages.

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