Aryl phosphate derivatives of AZT having anti-HIV activity
AssigneeParker Hughes Institute
InventorsFaith M. Uckun, Rakesh Vig
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Abstract
Aryl phosphate derivatives of d4T with para-bromo substitution on the aryl group show markedly increased potency as anti-HIV agents without undesirable levels of cytotoxic activity. In particular, these derivatives are potent inhibitors of HIV reverse transcriptase. In a preferred aspect of the present invention, the phosphorus of the aryl phosphate group is further substituted with an amino acid residue that may be esterified or substituted, such as a methoxy alaninyl group.
Claims16
A compound of the formula:
- wherein X is an electron withdrawing group, with the proviso that X is not NO2 or F;
- and R2 is an amino acid residue;
- or a pharmaceutically acceptable salt or ester thereof.
A method for inhibiting virus replication in a cell infected with a virus, the method comprising administering to the infected cell a virus replication inhibiting amount of a compound of the formula:
- wherein X is an electron withdrawing group, with the proviso that X is not NO2 or F;
- and R2 is an amino acid residue;
- or a pharmaceutically acceptable salt or ester thereof.
A composition useful for inhibiting virus replication in a cell infected with virus, the composition comprising an amount effective for inbibiting virus replication in the infected cell of a compound of the formula:
- wherein X is an electron withdrawing group, with the proviso that X is not NO2 or F;
- and R2 is an amino acid residue;
- or a pharmaceutically acceptable salt or ester thereof;
- and
- a pharmaceutically acceptable carrier, adjuvant or diluent.
Dependencies are inferred from the claim text.