Journal of pharmaceutical sciences

A novel prodrug strategy for β??dicarbonyl carbon acids: Syntheses and evaluation of the physicochemical characteristics of C??phosphoryloxymethyl (POM) and …

SS Dhareshwar, VJ Stella

Index: Dhareshwar, Sundeep S.; Stella, Valentino J. Journal of Pharmaceutical Sciences, 2010 ,  vol. 99,  # 6  p. 2711 - 2723

Full Text: HTML

Citation Number: 8

Abstract

Abstract The C-phosphoryloxymethyl (POM) and phosphoryloxymethyloxymethyl (POMOM) prodrugs resulting from derivatization at the reactive α-carbon of β-dicarbonyl carbon acid drugs represent a unique approach for improving their chemical stability and aqueous solubility. This work evaluates the physicochemical and in vitro enzymatic bioconversion lability of selected prodrugs of phenylbutazone and phenindione. The POM and POMOM ...