Anti-HIV-1 activities and pharmacokinetics of new arylpiperazinyl fluoroquinolones

Bioorg Med Chem Lett. 2002 Mar 11;12(5):739-42. doi: 10.1016/s0960-894x(02)00003-3.

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.

Publication types

  • Comparative Study

MeSH terms

  • Administration, Oral
  • Animals
  • Anti-HIV Agents / pharmacokinetics*
  • Anti-HIV Agents / pharmacology*
  • Biological Availability
  • Chlorofluorocarbons, Methane / chemistry
  • Fluoroquinolones / pharmacokinetics*
  • Fluoroquinolones / pharmacology*
  • HIV-1 / drug effects*
  • Macaca fascicularis
  • Molecular Structure
  • Rats
  • Structure-Activity Relationship
  • Virus Replication / drug effects

Substances

  • Anti-HIV Agents
  • Chlorofluorocarbons, Methane
  • Fluoroquinolones
  • fluoroform