Wake promoting agents: search for next generation modafinil, lessons learned: part III

Bioorg Med Chem Lett. 2012 Jun 1;22(11):3751-3. doi: 10.1016/j.bmcl.2012.04.031. Epub 2012 Apr 13.

Abstract

In searching for a next generation molecule to the novel wake promoting agent modafinil (compound 1), a series of fluorene-derived wakefulness enhancing agents were developed and evaluated in rat. Extensive pharmacokinetic studies of a potent member of the series (compound 15) revealed that the wake promotion activity of the analog was likely due to an active metabolite (compound 3).

MeSH terms

  • Animals
  • Benzhydryl Compounds / chemical synthesis
  • Benzhydryl Compounds / chemistry*
  • Benzhydryl Compounds / pharmacokinetics
  • Brain / drug effects
  • Brain / metabolism
  • Fluorenes / chemical synthesis
  • Fluorenes / chemistry*
  • Fluorenes / pharmacokinetics
  • Injections, Intraperitoneal
  • Modafinil
  • Neuroprotective Agents / chemical synthesis
  • Neuroprotective Agents / chemistry*
  • Neuroprotective Agents / pharmacokinetics
  • Rats
  • Sulfoxides / chemical synthesis
  • Sulfoxides / chemistry*
  • Sulfoxides / pharmacokinetics

Substances

  • Benzhydryl Compounds
  • Fluorenes
  • Neuroprotective Agents
  • Sulfoxides
  • fluoren-9-ol
  • Modafinil