Synthesis and immunosuppressive activity evaluation of substituted N-imidazolidin-2-ones and N-tetrahydropyrimidin-2(1H)-ones

J Enzyme Inhib Med Chem. 2008 Oct;23(5):659-67. doi: 10.1080/14756360802205455.

Abstract

Seventeen compounds with either an imidazolin-2-one or a tetrahydropyrimidin-2(1H)-one scaffold were synthesized and evaluated for their immunosuppressive activity in a concanavallin A (ConA)-stimulated mouse splenocytes proliferation test. Three of these molecules exerted a significant activity at 90 microM. All the compounds of the tetrahydropyrimidin-2(1H)-one series have turned out to be inactive showing the crucial role of the imidazolidin-2-one scaffold in the induction of an immunosuppressive activity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cell Proliferation
  • Concanavalin A / pharmacology
  • Imidazolidines / chemical synthesis
  • Imidazolidines / pharmacology*
  • Immunosuppressive Agents / chemical synthesis*
  • Mice
  • Mice, Inbred C57BL
  • Pyrimidinones / chemical synthesis
  • Pyrimidinones / pharmacology*
  • Spleen / cytology
  • Structure-Activity Relationship

Substances

  • Imidazolidines
  • Immunosuppressive Agents
  • Pyrimidinones
  • tetrahydropyrimidinone
  • Concanavalin A