Design of novel CXCR4 antagonists that are potent inhibitors of T-tropic (X4) HIV-1 replication

Bioorg Med Chem Lett. 2011 Mar 1;21(5):1414-8. doi: 10.1016/j.bmcl.2011.01.021. Epub 2011 Jan 11.

Abstract

A novel series of CXCR4 antagonists were identified based on the substantial redesign of AMD070. These compounds possessed potent anti-HIV-1 activity and showed excellent pharmacokinetics in rat and dog.

MeSH terms

  • Aminoquinolines
  • Animals
  • Anti-HIV Agents / chemical synthesis*
  • Anti-HIV Agents / chemistry
  • Anti-HIV Agents / pharmacokinetics
  • Benzimidazoles
  • Butylamines
  • DNA Replication / drug effects
  • Dogs
  • Drug Design*
  • HIV-1 / drug effects*
  • HIV-1 / physiology
  • Heterocyclic Compounds, 1-Ring / chemistry
  • Molecular Structure
  • Rats
  • Receptors, CXCR4 / antagonists & inhibitors*
  • Virus Replication / drug effects*

Substances

  • Aminoquinolines
  • Anti-HIV Agents
  • Benzimidazoles
  • Butylamines
  • Heterocyclic Compounds, 1-Ring
  • Receptors, CXCR4
  • mavorixafor