Document Report Card

ID: ALA1148294

Journal: J Med Chem

Title: Synthesis, in vitro evaluation, and antileishmanial activity of water-soluble prodrugs of buparvaquone.

Authors: Mäntylä A, Garnier T, Rautio J, Nevalainen T, Vepsälainen J, Koskinen A, Croft SL, Järvinen T.

Abstract: Water-soluble phosphate prodrugs of buparvaquone (1), containing a hydroxynaphthoquinone structure, were synthesized and evaluated in vitro for improved topical and oral drug delivery against cutaneous and visceral leishmaniasis. The successful prodrug synthesis involved a strong base; e.g., sodium hydride. Buparvaquone-3-phosphate (4a) and 3-phosphonooxymethyl-buparvaquone (4b) prodrugs possessed significantly higher aqueous solubilities (>3.5 mg/mL) than the parent drug (

CiteXplore: 14695832

DOI: 10.1021/jm030868a