title: Syntheses of Siderophore-Drug Conjugates Using a Convergent Thiol-Maleimide System.
abstract: Three siderophore-drug conjugates (sideromycins) were synthesized by preparation of a maleimide linked derivative of the siderophore desferrioxamine B and reacting the corresponding Ga(3+)-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 synthesis and screening of novel sideromycins.
authors.affiliation: Department of Chemistry and Biochemistry, 251 Nieuwland Science Hall, University of Notre Dame, Notre Dame, IN 46556, USA.
authors.forename: Raúl E
authors.initials: RE
authors.lastname: Juárez-Hernández
authors.forename: Patricia A
authors.initials: PA
authors.lastname: Miller
authors.forename: Marvin J
authors.initials: MJ
authors.lastname: Miller