Abstract
Styrylquinazoline derivatives were prepared by Perkin condensation and evaluated for inhibitory activity against HIV-1 integrase. Among them, compound 5c containing a free catechol ring was the most potent (IC(50)=0.8 +/- 1.9 microM)and showed 6-fold more potency than the corresponding styrylquinoline compound (IC(50) = 130.7 +/- 8.6 microM).
MeSH terms
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HIV Integrase Inhibitors / chemistry
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HIV Integrase Inhibitors / pharmacology*
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HIV-1 / enzymology*
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Humans
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Indicators and Reagents
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Magnetic Resonance Spectroscopy
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Mass Spectrometry
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Oligonucleotides / chemistry
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Quinazolines / chemical synthesis*
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Quinazolines / pharmacology*
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Structure-Activity Relationship
Substances
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HIV Integrase Inhibitors
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Indicators and Reagents
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Oligonucleotides
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Quinazolines