Aryl phosphate derivatives of d4T having anti-HIV activity
AssigneeParker Hughes Institute
InventorsFatih 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.
Claims20
A method for inhibiting HIV reverse transcriptase in cells infected with HIV, comprising administering to the infected cells an inhibiting amount of a compound of formula I or II, where X is an electron withdrawing group:
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A method for inhibiting HIV reverse transcriptase in cells infected with HIV, comprising administering to the infected cells an inhibiting amount of a compound of formula III, where X is an electron withdrawing group, and where R2 is an amino acid residue:
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A composition comprising a compound of formula I or II, where X is an electron withdrawing group:
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A composition comprising a compound of formula III, wherein R2 is an amino acid residue:
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A method for inhibiting HIV replication in a host cell, comprising contacting the host cell with an inhibiting amount of a compound of formula I or II, where X is an electron withdrawing group:
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A method for inhibiting HIV replication in host cells, comprising administering to the cells an inhibiting amount of a compound of formula III, where X is an electron withdrawing group, and where R2 is an amino acid residue:
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A composition comprising a compound of formula IV where X is an electron-withdrawing group substituted in the para or ortho position:
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Dependencies are inferred from the claim text.