Abstract
Anti-HIV-1 activities and pharmacokinetics of a series of novel arylpiperazinyl fluoroquinolones are reported. Modification at the C-8 position with a trifluoromethyl group was superior to that with a difluoromethoxy group to achieve higher anti-HIV-1 activity. Two compounds studied exhibited quite high anti-HIV-1 activities (IC(50)<50 nM) in vitro and high bioavailabilities (BA>90%) in monkeys.
MeSH terms
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Administration, Oral
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Animals
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Anti-HIV Agents / pharmacokinetics*
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Anti-HIV Agents / pharmacology*
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Biological Availability
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Chlorofluorocarbons, Methane / chemistry
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Fluoroquinolones / pharmacokinetics*
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Fluoroquinolones / pharmacology*
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HIV-1 / drug effects*
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Macaca fascicularis
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Molecular Structure
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Rats
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Structure-Activity Relationship
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Virus Replication / drug effects
Substances
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Anti-HIV Agents
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Chlorofluorocarbons, Methane
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Fluoroquinolones
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fluoroform