Design, synthesis, and anticonvulsant activity of some sulfamides

Bioorg Med Chem. 2007 Aug 15;15(16):5604-14. doi: 10.1016/j.bmc.2007.05.024. Epub 2007 May 17.

Abstract

As part of our search for potential anticonvulsant agents, a set of compounds were designed, synthesized, and evaluated against MES and PTZ tests. Bioisosteric functional group information was used to design a new functionality, sulfamides, that complies with the requirements of the pharmacophore previously defined. Some of the molecules showed a promising anticonvulsant profile as selective anti-MES drugs, being active at low concentrations (30mg/kg). The biological data were confirmed in Phase II of the Anticonvulsant Drug Development Program of the National Institute of Health.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amides / chemical synthesis
  • Amides / chemistry*
  • Amides / pharmacology*
  • Animals
  • Anticonvulsants / chemical synthesis*
  • Anticonvulsants / chemistry
  • Anticonvulsants / pharmacology*
  • Drug Design*
  • Electrons
  • Male
  • Mice
  • Models, Molecular
  • Molecular Structure
  • Structure-Activity Relationship
  • Sulfur / chemistry*

Substances

  • Amides
  • Anticonvulsants
  • Sulfur