期刊
JOURNAL OF MEDICAL MICROBIOLOGY
卷 55, 期 4, 页码 407-415出版社
MICROBIOLOGY SOC
DOI: 10.1099/jmm.0.46319-0
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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 mu g ml(-1)) for several clinical isolates, whilst having low toxicity for THP-1 monocytes and macrophages.
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