Structure-activity relationship studies on unifiram (DM232) and sunifiram (DM235), two novel and potent cognition enhancing drugs

Bioorg Med Chem. 2004 Jan 2;12(1):71-85. doi: 10.1016/j.bmc.2003.10.025.

Abstract

Structure-activity relationships on two novel potent cognition enhancing drugs, unifiram (DM232, 1) and sunifiram (DM235, 2), are reported. Although none of the compounds synthesised reached the potency of the parent drugs, some fairly active compounds have been identified that may represent new leads to develop other cognition enhancing drugs. An interesting result of this research is the identification of two compounds (13 and 14) that are endowed with amnesing activity (the opposite of the activity of the original molecules) and are nearly equipotent to scopolamine. Moreover, two compounds of the series (5 and 6) were found endowed with analgesic activity on a rat model of neuropathic pain at the dose of 1 mg/kg.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Avoidance Learning / drug effects
  • Avoidance Learning / physiology
  • Dose-Response Relationship, Drug
  • Mice
  • Nootropic Agents / chemistry*
  • Nootropic Agents / pharmacology
  • Pain Measurement / drug effects
  • Pain Measurement / methods
  • Pain Threshold / drug effects
  • Piperazines / chemistry*
  • Piperazines / pharmacology
  • Pyrroles / chemistry*
  • Pyrroles / pharmacology
  • Rats
  • Structure-Activity Relationship

Substances

  • Nootropic Agents
  • Piperazines
  • Pyrroles
  • DM 235
  • DM 232