Synthesis and biological evaluation of a water-soluble derivative of the potent V-ATPase inhibitor archazolid

The water-solubility of the highly potent V-ATPase inhibitors archazolid A and the glucosylated derivative archazolid C was studied in the presence of a wide range of cosolvents, revealing very low solubilites. The first water-soluble analogue was then designed, synthesized, and evaluated for V-ATPa...

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Hauptverfasser: Persch, Elke (VerfasserIn) , Menche, Dirk (VerfasserIn)
Dokumenttyp: Article (Journal)
Sprache:Englisch
Veröffentlicht: 13 October 2012
In: Bioorganic & medicinal chemistry letters
Year: 2012, Jahrgang: 22, Heft: 24, Pages: 7735-7738
ISSN:1464-3405
DOI:10.1016/j.bmcl.2012.09.081
Online-Zugang:Verlag, Volltext: http://dx.doi.org/10.1016/j.bmcl.2012.09.081
Verlag, Volltext: http://www.sciencedirect.com/science/article/pii/S0960894X1201236X
Volltext
Verfasserangaben:Elke Persch, Teodora Basile, Svenja Bockelmann, Markus Huss, Helmut Wieczorek, Teresa Carlomagno, Dirk Menche
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Zusammenfassung:The water-solubility of the highly potent V-ATPase inhibitors archazolid A and the glucosylated derivative archazolid C was studied in the presence of a wide range of cosolvents, revealing very low solubilites. The first water-soluble analogue was then designed, synthesized, and evaluated for V-ATPase inhibitory activity in vitro.
Beschreibung:Gesehen am 19.07.2018
Beschreibung:Online Resource
ISSN:1464-3405
DOI:10.1016/j.bmcl.2012.09.081