Hydroxamate analog libraries and evaluation of their iron affinity

Słomczyńska, Urszula; Reddy, P. A.; Schall, Otto F.; Rosik, Leonard O.; Wheatley, James R.; Marshall, Garland R.

doi:10.1016/s0955-3886(00)00104-1

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“…To assess the impact of structural variation on ferric ion affinity, a high-throughput screening assay was developed, the details of which are also discussed. Some of these results were presented at various meetings, , and an overview has appeared in a review…”

Section: Introductionmentioning

confidence: 99%

Hydroxamate-Based Iron Chelators: Combinatorial Syntheses of Desferrioxamine B Analogues and Evaluation of Binding Affinities

Poreddy¹,

Schall²,

Osiek³

et al. 2004

J. Comb. Chem.

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This article describes the solid-phase combinatorial methods developed for the synthesis of polyhydroxamate-based siderophores. This strategy was applied to generate several libraries of structural DFO (1a) analogues that include DFO variants, non-amide analogues, C-terminal modified analogues, reverse-amide analogues, and hybrid analogues. To assess the relative iron-binding affinities of these compounds, a high-throughput spectrophotometric screening method based on competition with 8-hydroxyquinoline-5-sulfonic acid was developed. Some of the promising candidates containing various terminal functional groups were identified and prepared on large scale to enable future studies in animal models for iron-overload diseases.

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Section: Introductionmentioning

confidence: 99%