Structure-activity relationship study on anti-HIV 6-desfluoroquinolones

J Med Chem. 2008 Sep 11;51(17):5454-8. doi: 10.1021/jm701585h. Epub 2008 Aug 19.

Abstract

On the basis of our recent findings that 6-aminoquinolones inhibit the HIV Tat-mediated transactivation, we have designed a broad series of derivatives identifying novel potent agents such as the 6-desfluoroquinolones 24 (HM12) and 27 (HM13), which showed pronounced anti-HIV activity in acutely, chronically, and latently HIV-1 infected cell cultures. We demonstrate here that highly potent molecules can be obtained by optimizing the substituent in the various positions of the quinolone nucleus.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-HIV Agents / chemistry*
  • Anti-HIV Agents / pharmacology
  • Cells, Cultured
  • HIV Infections / drug therapy
  • HIV-1 / drug effects
  • Humans
  • Quinolines / chemistry
  • Quinolines / pharmacology*
  • Quinolones
  • Structure-Activity Relationship

Substances

  • Anti-HIV Agents
  • HM-12 compound
  • Quinolines
  • Quinolones