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

E Persch, T Basile, S Bockelmann, M Huss, H Wieczorek, T Carlomagno & D Menche

Bioorganic & Medicinal Chemistry Letters

Pages
7735–7738
Issue
24
Volume
22
Year
2012

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.