Abstract
A novel series of HIV-1 integrase inhibitors was synthesized and tested in both in vitro and ex vivo assays. These inhibitors are featured by the presence of a quinoline subunit and an ancillary aromatic ring linked by functionalized spacers such as amide, hydrazide, urea and 1-hydroxyprop-1-en-3-one moiety. Amide derivatives are the most promising ones and could serve as leads for further developments.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Cell Line
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Cell Survival / drug effects
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Cross-Linking Reagents
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HIV Infections / drug therapy
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HIV Integrase / drug effects
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HIV Integrase Inhibitors / chemical synthesis*
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HIV Integrase Inhibitors / pharmacology
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Humans
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Inhibitory Concentration 50
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Quinolines / chemical synthesis
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Quinolines / pharmacology*
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Structure-Activity Relationship
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Virion / drug effects
Substances
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Cross-Linking Reagents
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HIV Integrase Inhibitors
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Quinolines
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HIV Integrase