N-hydroxymethyl derivatives of nitrogen heterocycles as possible prodrugs II: possible prodrugs of allopurinol, glutethimide, and phenobarbital.

Abstract

Solid samples of 1-hydroxymethyl- and 1,5-dihydroxymethylallopurinol, 1-hydroxymethylglutethimide, and 1-hydroxymethylphenobarbital were prepared, and equilibrium constants for their formation from formaldehyde and allopurinol, glutethimide, or phenobarbital were calculated. The N-hydroxymethyl derivatives had higher water solubilities and faster dissolution rates than the parent drugs, and they appear to be potentially useful as prodrugs.

Cite this paper

@article{Bansal1981NhydroxymethylDO, title={N-hydroxymethyl derivatives of nitrogen heterocycles as possible prodrugs II: possible prodrugs of allopurinol, glutethimide, and phenobarbital.}, author={Pansy Bansal and Ivan Pitman and Takashi Higuchi}, journal={Journal of pharmaceutical sciences}, year={1981}, volume={70 8}, pages={855-7} }