Design, synthesis and preliminary pharmacological evaluation of new analogues of DM232 (unifiram) and DM235 (sunifiram) as cognition modulators

Bioorg Med Chem. 2008 Dec 1;16(23):10034-42. doi: 10.1016/j.bmc.2008.10.017. Epub 2008 Oct 11.

Abstract

A series of amides, structurally related to DM232 (unifiram) and DM235 (sunifiram), characterized by a 1,2,3,4-tetrahydropyrazino[2,1-a]isoindol-6(2H)-one, 1,4-diamino-cyclohexane or 1,4-diaminobenzene ring, have been synthesized and tested for cognition-enhancing activity in the mouse passive-avoidance test. Some of the compounds display good antiamnesic and procognitive activity, with higher potency than piracetam, while some cyclohexane derivatives are endowed with amnesia inducing properties.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Avoidance Learning / drug effects
  • Avoidance Learning / physiology
  • Data Interpretation, Statistical
  • Drug Design
  • Mice
  • Nootropic Agents / chemical synthesis*
  • Nootropic Agents / chemistry
  • Nootropic Agents / pharmacology*
  • Piperazines / chemistry*
  • Piperazines / pharmacology
  • Pyrroles / chemistry*
  • Pyrroles / pharmacology
  • Recognition, Psychology / drug effects

Substances

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