Abstract
Novel non-nucleoside inhibitors of HIV-RT that contain pyridazinone isosteres were prepared, and a series of triazolinones were found to be potent inhibitors of HIV replication. These compounds were active against several NNRTI-resistant virus strains. Pharmacokinetic studies indicated that inhibitor 7e has good bioavailability in rats. Several fragments of inhibitor 7c were prepared, and the binding of these compounds to HIV-RT was analyzed by surface plasmon resonance spectroscopy.
MeSH terms
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Animals
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Anti-HIV Agents* / chemical synthesis
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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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Combinatorial Chemistry Techniques
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Drug Resistance, Viral / drug effects
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Molecular Structure
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Pyridazines* / chemical synthesis
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Pyridazines* / chemistry
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Pyridazines* / pharmacokinetics
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Pyridazines* / pharmacology
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Rats
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Reverse Transcriptase Inhibitors* / chemical synthesis
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Reverse Transcriptase Inhibitors* / chemistry
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Reverse Transcriptase Inhibitors* / pharmacology
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Structure-Activity Relationship
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Surface Plasmon Resonance
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Triazoles* / chemical synthesis
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Triazoles* / chemistry
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Triazoles* / pharmacokinetics
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Triazoles* / pharmacology
Substances
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Anti-HIV Agents
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Pyridazines
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Reverse Transcriptase Inhibitors
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Triazoles