Monodisperse oligoethylene glycols modified Propofol prodrugs

Bioorg Med Chem Lett. 2018 Dec 1;28(22):3502-3505. doi: 10.1016/j.bmcl.2018.10.009. Epub 2018 Oct 10.

Abstract

The low water solubility of Propofol resulted in complicated formulation and adverse effects during its clinical application. To improve its water solubility and maintain its anesthetic effects, Propofol prodrugs with monodisperse oligoethylene glycols as solubility enhancer were designed and synthesized. Monodisperse oligoethylene glycols enable the concise manipulation of water solubility, biocompatibility and anesthetic effects. Through the physicochemical and biological assay, a few water soluble prodrugs of Propofol were identified as promising anesthetic to overcome the drawbacks associated with Propofol.

Keywords: Anesthetic; Monodisperse; Polyethylene glycols; Prodrug; Propofol.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anesthetics / blood
  • Anesthetics / chemistry*
  • Anesthetics / pharmacology
  • Animals
  • Cell Line
  • Cell Survival / drug effects
  • Humans
  • Polyethylene Glycols / chemistry*
  • Prodrugs / chemical synthesis
  • Prodrugs / chemistry*
  • Prodrugs / pharmacology
  • Propofol / blood
  • Propofol / chemistry*
  • Propofol / pharmacology
  • Rats
  • Rats, Sprague-Dawley
  • Solubility

Substances

  • Anesthetics
  • Prodrugs
  • Polyethylene Glycols
  • Propofol