Carbohydrate-Based Macrolides Prepared via a Convergent Ring Closing Metathesis Approach:  In Search for Novel Antibiotics

An efficient convergent approach has been developed for the construction of novel, nonnatural polysubstituted carbohydrate-based macrolides. A key step in the synthesis is the formation of the macrocyclic ring via a ring-closing metathesis reaction. The obtained macrolide analogues have been screene...

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Veröffentlicht in:Journal of organic chemistry 2007-07, Vol.72 (15), p.5514-5522
Hauptverfasser: Ruttens, Bart, Blom, Petra, Van Hoof, Steven, Hubrecht, Idzi, Van der Eycken, Johan, Sas, Benedikt, Van hemel, Johan, Vandenkerckhove, Jan
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Sprache:eng
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Zusammenfassung:An efficient convergent approach has been developed for the construction of novel, nonnatural polysubstituted carbohydrate-based macrolides. A key step in the synthesis is the formation of the macrocyclic ring via a ring-closing metathesis reaction. The obtained macrolide analogues have been screened for biological activity against gram-positive and gram-negative bacteria, yeasts, and molds.
ISSN:0022-3263
1520-6904
DOI:10.1021/jo061929q