Synthesis and biological evaluation of a water-soluble derivative of the potent V-ATPase inhibitor archazolid
Authors: Persch E, Basile T, Bockelmann S, Huss M, Wieczorek H, Carlomagno T, Menche D
CellNetworks People: Carlomagno Teresa
Journal: Bioorg Med Chem Lett.

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.