Preparation of a 3'-azido-3'-deoxythymidine (AZT) derivative, which is blood-brain barrier permeable

Chem Commun (Camb). 2009 Aug 21:(31):4669-71. doi: 10.1039/b909541a. Epub 2009 Jun 22.

Abstract

The anti-AIDS drug AZT was covalently attached to the recently reported sorbitol-G8 transporter, and the conjugate was found to target mitochondria in HeLa cells and readily cross the blood-brain barrier (BBB) to gain access into the mouse brain, suggesting the potential of these molecular transporters as practical central nervous system (CNS) delivery vectors.

MeSH terms

  • Animals
  • Anti-HIV Agents / chemical synthesis*
  • Anti-HIV Agents / chemistry
  • Anti-HIV Agents / metabolism
  • Blood-Brain Barrier*
  • HeLa Cells
  • Humans
  • Mice
  • Microscopy, Confocal
  • Mitochondria / drug effects*
  • Molecular Structure
  • Permeability
  • Zidovudine / chemical synthesis*
  • Zidovudine / chemistry
  • Zidovudine / metabolism

Substances

  • Anti-HIV Agents
  • Zidovudine