Heteroatom analogues of hydrocodone: synthesis and biological activity

J Org Chem. 2013 Apr 5;78(7):2914-25. doi: 10.1021/jo3026753. Epub 2013 Mar 6.

Abstract

Heteroatom analogues of hydrocodone, in which the N-methyl functionality was replaced with oxygen, sulfur, sulfoxide, and sulfone, were prepared by a short sequence from the ethylene glycol ketal of hydrocodone; a carbocyclic analogue of bisnorhydrocodone was also prepared. The compounds were tested for receptor binding and revealed moderate levels of activity for the sulfone analogue of hydrocodone.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • CHO Cells
  • Cricetinae
  • Cyclization
  • Dose-Response Relationship, Drug
  • Humans
  • Hydrocodone / chemical synthesis*
  • Hydrocodone / chemistry
  • Hydrocodone / pharmacology*
  • Molecular Structure
  • Narcotic Antagonists*
  • Structure-Activity Relationship

Substances

  • Narcotic Antagonists
  • Hydrocodone