【摘 要】
：
The anthrax lethal factor (LF),a Zn-dependent endopeptidase,has a major role in the development and virulence of anthrax,an infectious disease caused by the toxigenic bacterium Bacillus anthracis. Con
【机 构】
：
Department of Chemistry and Institute of Catalysis Science and Technology，Israel
【出 处】
：
2005 WHTS3rd Annual Congress of International Drug Discovery
论文部分内容阅读
The anthrax lethal factor (LF),a Zn-dependent endopeptidase,has a major role in the development and virulence of anthrax,an infectious disease caused by the toxigenic bacterium Bacillus anthracis. Consequently,an intensive search for specific inhibitors of LF has been performed during the last years. Neomycin B,a commonly utilized aminoglycoside antibiotic,was found to be the most potent inhibitor of LF. In attempts to improve the inhibitory effect of neomycin B derivatives,we synthesized a series of new derivatives of neomycin B. which represent a new class of branched aminoglycosides that show dual effect by inhibiting LF at seemingly physiological conditions and simultaneously are active against B. anthracis. A11 new derivatives are competitive inhibitors of LF with improved activity of up to 53-times better than neomycin B. As such,this study provides a new direction for the development of novel antibiotics that target at once both the toxigenic bacterium and its released lethal toxin,and may offer promise for the effective treatment of anthrax infection. Selected compounds of this series also show antibacterial activity superior to that of neomycin B against resistant strains of Pseudomonas aeruginosa,the major cause of morbidity and mortality in cystic fibrosis patients. Most recent results in these issues will be discussed.
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