Syntheses of Siderophore–Drug Conjugates Using a Convergent Thiol–Maleimide System
Authors:
- 11 September 2012
- journal article
- research article
- Published by American Chemical Society (ACS) in ACS Medicinal Chemistry Letters
- Vol. 3 (10) , 799-803
Abstract
Three siderophore–drug conjugates (sideromycins) were synthesized by preparation of a maleimide linked derivative of the siderophore desferrioxamine B and reacting the corresponding Ga3+-complex with freshly prepared thiol-containing antibiotics: loracarbef, ciprofloxacin, and nadifloxacin. The conjugates and their synthetic precursors were tested against a broad panel of bacteria and were found to display Gram-positive selective, growth inhibitory activity (μM), indicating that this approach is suitable for the convergent syntheses and screening of novel sideromycins.Keywords
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