Piperazine derivatives with central pharmacological activity used as therapeutic tools

Fundam Clin Pharmacol. 2019 Feb;33(1):13-24. doi: 10.1111/fcp.12408. Epub 2018 Sep 17.

Abstract

Medicinal chemistry is a science applied to the search and discovery of new therapeutic agents for the treatment of various diseases. Therefore, promising structures have been identified; one of these structures is the piperazine moiety, a cyclic molecule containing two nitrogen atoms in positions 1 and 4 as well as four carbon atoms. Many piperazine derivatives have central pharmacological activity that mainly involves the activation of the monoamine pathway. Thus, piperazine derivatives have been the subject of research for many central therapeutic applications, including antipsychotic, antidepressant and anxiolytic applications. Benzylpiperazine is the prototype of piperazine derivatives; this substance is the main component of recreational drugs, partly due to its stimulant and euphoric effects. This paper describes some piperazine derivatives used therapeutically as antipsychotic (clozapine), antidepressant (vortioxetine) and anxiolytic (buspirone) drugs.

Keywords: Antidepressant; Anxiolytic; Medicinal chemistry; Neuropharmacology.

Publication types

  • Review

MeSH terms

  • Anti-Anxiety Agents / chemistry
  • Anti-Anxiety Agents / pharmacology
  • Antidepressive Agents / chemistry
  • Antidepressive Agents / pharmacology
  • Antipsychotic Agents / chemistry
  • Antipsychotic Agents / pharmacology
  • Chemistry, Pharmaceutical / methods*
  • Drug Discovery / methods*
  • Humans
  • Piperazines / chemistry
  • Piperazines / pharmacology*

Substances

  • Anti-Anxiety Agents
  • Antidepressive Agents
  • Antipsychotic Agents
  • Piperazines
  • 1-benzylpiperazine