Chromones: A Promising Ring System for New Anti-inflammatory Drugs

ChemMedChem. 2016 Oct 19;11(20):2252-2260. doi: 10.1002/cmdc.201600359. Epub 2016 Sep 15.

Abstract

The quest for safer anti-inflammatory drugs is still the focus of several medicinal chemistry programs. Chromones (4H-chromen-4-ones) are a group of naturally occurring compounds ubiquitous in plants, and the chromone core has proven to be a privileged scaffold in medicinal chemistry. Herein we provide an overview of the relevance of chromones as anti-inflammatory agents, specifically as inhibitors of cyclooxygenase (COX), 5-lipoxygenase (5-LOX), interleukin-5 (IL-5), and nitric oxide (. NO) production. Numerous structure-activity relationships and mechanisms of action are discussed. This review is therefore intended to provide a foundation for the design and synthesis of novel chromone-based compound libraries for further development into safer and more efficient anti-inflammatory agents.

Keywords: anti-inflammatory agents; chromones; mechanism of action; structure-activity relationships.

Publication types

  • Review
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Inflammatory Agents, Non-Steroidal / chemical synthesis
  • Anti-Inflammatory Agents, Non-Steroidal / chemistry*
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
  • Arachidonate 5-Lipoxygenase / metabolism
  • Chromones / chemistry
  • Chromones / pharmacology*
  • Cyclooxygenase Inhibitors / chemistry
  • Cyclooxygenase Inhibitors / pharmacology*
  • Drug Design*
  • Interleukin-5 / antagonists & inhibitors
  • Interleukin-5 / biosynthesis
  • Lipoxygenase Inhibitors / chemistry
  • Lipoxygenase Inhibitors / pharmacology*
  • Molecular Structure
  • Nitric Oxide / antagonists & inhibitors
  • Nitric Oxide / biosynthesis
  • Prostaglandin-Endoperoxide Synthases / metabolism
  • Structure-Activity Relationship

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Chromones
  • Cyclooxygenase Inhibitors
  • Interleukin-5
  • Lipoxygenase Inhibitors
  • Nitric Oxide
  • Arachidonate 5-Lipoxygenase
  • Prostaglandin-Endoperoxide Synthases