title: Chromones: A Promising Ring System for New Anti-inflammatory Drugs.
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.
authors.affiliation: Department of Chemistry & QOPNA, University of Aveiro, Campus Universitário de Santiago, 3810-193, Aveiro, Portugal.
authors.forename: Carlos F M
authors.initials: CF
authors.lastname: Silva
authors.affiliation: Department of Chemistry & QOPNA, University of Aveiro, Campus Universitário de Santiago, 3810-193, Aveiro, Portugal. diana@ua.pt.
authors.forename: Diana C G A
authors.identifier: 0000-0003-4249-7089
authors.initials: DC
authors.lastname: Pinto
authors.affiliation: Department of Chemistry & QOPNA, University of Aveiro, Campus Universitário de Santiago, 3810-193, Aveiro, Portugal.
authors.forename: Artur M S
authors.identifier: 0000-0003-2861-8286
authors.initials: AM
authors.lastname: Silva
mesh_terms: D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D001094:Arachidonate 5-Lipoxygenase / Q000378:metabolism; D002867:Chromones / Q000737:chemistry / Q000494:pharmacology*; D016861:Cyclooxygenase Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D015195:Drug Design; D015848:Interleukin-5 / Q000037:antagonists & inhibitors / Q000096:biosynthesis; D016859:Lipoxygenase Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D015394:Molecular Structure; D009569:Nitric Oxide / Q000037:antagonists & inhibitors / Q000096:biosynthesis; D011451:Prostaglandin-Endoperoxide Synthases / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D002867:Chromones; D016861:Cyclooxygenase Inhibitors; D015848:Interleukin-5; D016859:Lipoxygenase Inhibitors; D009569:Nitric Oxide; D001094:Arachidonate 5-Lipoxygenase; D011451:Prostaglandin-Endoperoxide Synthases
keywords: anti-inflammatory agents; chromones; mechanism of action; structure-activity relationships