Abstract
Two new phosphonate 3TC prodrugs were synthesized and studied in MT-4 cells as inhibitors of HIV replication. Their pharmacokinetic parameters were evaluated following intragastric administration in rabbits and oral administration in dogs. Both compounds were much less toxic than parent 3TC in cell cultures and could generate the active nucleoside in laboratory animals.
© 2011 John Wiley & Sons A/S.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Anti-HIV Agents / chemistry
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Anti-HIV Agents / pharmacokinetics
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Anti-HIV Agents / pharmacology*
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Cell Line
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Chromatography, High Pressure Liquid
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Dogs
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Drug Evaluation, Preclinical
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Female
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HIV-1 / drug effects
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HIV-1 / physiology
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Humans
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Lamivudine / chemistry
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Lamivudine / pharmacokinetics
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Lamivudine / pharmacology*
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Magnetic Resonance Spectroscopy
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Male
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Prodrugs / chemistry
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Prodrugs / pharmacokinetics
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Prodrugs / pharmacology*
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Rabbits
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Virus Replication / drug effects
Substances
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Anti-HIV Agents
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Prodrugs
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Lamivudine