Synthesis and biological evaluation of new heterocyclic quinolinones as anti-parasite and anti-HIV drug candidates

Bioorg Med Chem Lett. 2009 Oct 15;19(20):5962-4. doi: 10.1016/j.bmcl.2009.08.013. Epub 2009 Aug 7.

Abstract

We have synthesized quinolinones with potential antiparasitic and anti-HIV activities by an original two-step method involving microwave irradiation and have evaluated their activities against Plasmodium falciparum, Leishmania donovani, Trichomonas vaginalis, and HIV. None of the tested compounds had been previously described using this method of synthesis. One of the compounds had interesting antiparasitic and anti-HIV activity, which could be improved by substitution with different radicals.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-HIV Agents / chemical synthesis*
  • Anti-HIV Agents / chemistry
  • Anti-HIV Agents / toxicity
  • Antiparasitic Agents / chemical synthesis*
  • Antiparasitic Agents / chemistry
  • Antiparasitic Agents / toxicity
  • Heterocyclic Compounds, 3-Ring / chemical synthesis*
  • Heterocyclic Compounds, 3-Ring / chemistry
  • Heterocyclic Compounds, 3-Ring / toxicity
  • Humans
  • Leishmania donovani / drug effects
  • Monocytes / drug effects
  • Monocytes / immunology
  • Parasitic Sensitivity Tests
  • Plasmodium falciparum / drug effects
  • Quinolones / chemical synthesis*
  • Quinolones / chemistry
  • Quinolones / toxicity
  • Trichomonas vaginalis / drug effects

Substances

  • Anti-HIV Agents
  • Antiparasitic Agents
  • Heterocyclic Compounds, 3-Ring
  • Quinolones