Scientific Publications by FDA Staff
J Pharm Sci 1994 Sep;83(9):1269-73
Synthesis, hydrolytic behavior, and anti-HIV activity of selected acyloxyalkyl esters of trisodium phosphonoformate (foscarnet sodium).
Iyer RP, Boal JH, Phillips LR, Thakker DR, Egan W
The synthesis and anti-HIV activity of selected (acyloxy)alkyl esters of trisodium phosphonoformate (foscarnet sodium) are described. The conversion of bis(trimethylsilyl) (alkoxycarbonyl)phosphonates 11a-d to the corresponding disilver salts 12a-d and their subsequent reaction with iodoalkyl acrylates 4a-c gave the desired bis(acyloxyalkyl) phosphonates 6-9(a-c). Of the analogs tested, only the dichlorophenyl analog 9a showed a dose-dependent inhibition of HIV activity in H9 cells. Using 31P-NMR, bioreversibility has been investigated in an attempt to rationalize these results.
|Category: Journal Article|
|PubMed ID: #7530302||DOI: 10.1002/jps.2600830916|
|Includes FDA Authors from Scientific Area(s): Biologics|
|Entry Created: 2012-12-24|