Synthesis and in vivo evaluation of 3-substituted gababutins

Bioorg Med Chem Lett. 2010 Jan 1;20(1):362-5. doi: 10.1016/j.bmcl.2009.10.089. Epub 2009 Oct 25.

Abstract

A range of 3-alkylated five-membered ring derivatives of Gabapentin were synthesized and several were found to have good levels of potency against the alpha2delta calcium subunit of a voltage-gated calcium channel. Two compounds were profiled in in vivo models of pain and anxiety.

MeSH terms

  • Amines / chemical synthesis*
  • Amines / chemistry
  • Amines / pharmacology
  • Amino Acids / chemical synthesis*
  • Amino Acids / chemistry
  • Amino Acids / pharmacology
  • Animals
  • Anti-Anxiety Agents / chemical synthesis*
  • Anti-Anxiety Agents / chemistry
  • Anti-Anxiety Agents / pharmacology
  • Calcium Channels / metabolism
  • Carrageenan / pharmacology
  • Cyclohexanecarboxylic Acids / chemical synthesis*
  • Cyclohexanecarboxylic Acids / chemistry
  • Cyclohexanecarboxylic Acids / pharmacology
  • Cyclopentanes / chemical synthesis*
  • Cyclopentanes / chemistry
  • Cyclopentanes / pharmacology
  • Gabapentin
  • Hyperalgesia / chemically induced
  • Hyperalgesia / drug therapy
  • Rats
  • Stereoisomerism
  • gamma-Aminobutyric Acid / chemical synthesis*
  • gamma-Aminobutyric Acid / chemistry
  • gamma-Aminobutyric Acid / pharmacology

Substances

  • Amines
  • Amino Acids
  • Anti-Anxiety Agents
  • Calcium Channels
  • Cyclohexanecarboxylic Acids
  • Cyclopentanes
  • gamma-Aminobutyric Acid
  • Gabapentin
  • Carrageenan