4.5 Review

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

Journal

CHEMMEDCHEM
Volume 11, Issue 20, Pages 2252-2260

Publisher

WILEY-V C H VERLAG GMBH
DOI: 10.1002/cmdc.201600359

Keywords

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

Funding

  1. University of Aveiro
  2. Fundacao para a Ciencia e a Tecnologia (FCT) FCT/MEC [FCT UID/QUI/00062/2013]
  3. Fundo Europeu de Desenvolvimento Regional (FEDER)

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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)-N-center dot) 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.

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