Synthesis and Structure-Activity Relationship Studies of Anti-Inflammatory Epoxyisoprostane Analogues

Org Lett. 2018 May 18;20(10):3014-3016. doi: 10.1021/acs.orglett.8b01042. Epub 2018 May 8.

Abstract

The lactone derivative of the epoxyisoprostane EC is a highly effective inhibitor of the secretion of the proinflammatory cytokine IL-6. Herein, a modular synthesis of analogues is described, allowing flexible variations of the cyclic side chain of the parent lactone. A structure-activity relationship study identified a lactam analogue that retains the high activity. Furthermore, the exocyclic allylic alcohol was shown to be crucial for the observed effect.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Inflammatory Agents / chemical synthesis*
  • Cytokines
  • Epoxy Compounds / chemical synthesis*
  • Molecular Structure
  • Structure-Activity Relationship

Substances

  • Anti-Inflammatory Agents
  • Cytokines
  • Epoxy Compounds