Syntheses and optimization of new GS39783 analogues as positive allosteric modulators of GABA B receptors

Bioorg Med Chem Lett. 2007 Nov 15;17(22):6206-11. doi: 10.1016/j.bmcl.2007.09.023. Epub 2007 Sep 8.

Abstract

The optimization of GS39783 into potent, selective, and safe positive allosteric modulators of GABA(B) receptors is presented.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Allosteric Regulation
  • Cyclopentanes / chemical synthesis*
  • Cyclopentanes / chemistry
  • Cyclopentanes / pharmacology*
  • Drug Evaluation, Preclinical
  • Molecular Structure
  • Pyrimidines / chemical synthesis*
  • Pyrimidines / chemistry
  • Pyrimidines / pharmacology*
  • Receptors, GABA-B / chemistry
  • Receptors, GABA-B / drug effects*
  • Structure-Activity Relationship

Substances

  • Cyclopentanes
  • N,N'-dicyclopentyl-2-methylsulfanyl-5-nitro-pyrimidine-4,6-diamine
  • Pyrimidines
  • Receptors, GABA-B