Drug Development
Novel water-soluble buparvaquone prodrugs synthesized
Published in Drug Week, December 17th, 2004
In a recent study from Finland, a series of "water-soluble phosphate prodrugs (2b-5b) of buparvaquone-oxime (1a) and buparvaquone-O-methyloxime (1b) were synthesized and evaluated in vitro as potential oral prodrugs against leishmaniasis."
"Buparvaquone-oxime (1a), and most probably also buparvaquone-O-methyloxime (1b), released the parent buparvaquone via a cytochrome P450-catalyzed reaction," A. Mantyla and coauthors at the University of Kuopio found. "The prodrugs 2b-5b showed significantly higher aqueous solubilities (>4 mg/mL) than buparvaquone...
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Source: Drug Week (2004-12-17)
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