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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| Main Authors: | , |
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| Format: | Article (Journal) |
| Language: | English |
| Published: |
13 October 2012
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| In: |
Bioorganic & medicinal chemistry letters
Year: 2012, Volume: 22, Issue: 24, Pages: 7735-7738 |
| ISSN: | 1464-3405 |
| DOI: | 10.1016/j.bmcl.2012.09.081 |
| Online Access: | Verlag, Volltext: http://dx.doi.org/10.1016/j.bmcl.2012.09.081 Verlag, Volltext: http://www.sciencedirect.com/science/article/pii/S0960894X1201236X 
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| Author Notes: | Elke Persch, Teodora Basile, Svenja Bockelmann, Markus Huss, Helmut Wieczorek, Teresa Carlomagno, Dirk Menche |
| Summary: | 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. |
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| Item Description: | Gesehen am 19.07.2018 |
| Physical Description: | Online Resource |
| ISSN: | 1464-3405 |
| DOI: | 10.1016/j.bmcl.2012.09.081 |