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U.S. Department of Health and Human Services

Scientific Publications by FDA Staff

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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