Current progress on antioxidants incorporating the pyrazole core

• Published in: European journal of medicinal chemistry Vol. 156; pp. 394 - 429
• Main Authors: Silva, Vera L.M., Elguero, J., Silva, Artur M.S.
• Format: Journal Article
• Language: English
• Published: France Elsevier Masson SAS 05.08.2018
• Subjects: Animals; Antioxidant; Antioxidants - chemistry; Antioxidants - pharmacology; Dihydropyrazole; Drug Discovery - methods; Free radical; Humans; Nitrogen heterocycles; Oxidative stress; Oxidative Stress - drug effects; Pyrazole; Pyrazoles - chemistry; Pyrazoles - pharmacology; Structure-Activity Relationship; Oxidative stress; Nitrogen heterocycles; Antioxidant; Free radical; Pyrazole; Dihydropyrazole
• ISSN: 0223-5234; 1768-3254
• DOI: 10.1016/j.ejmech.2018.07.007

The search of new antioxidants, as drugs candidates, is an active field of medicinal chemistry. The synthesis of compounds with antioxidant potential has increased in recent years and a high number of structurally diverse compounds have been published. This review aims to show the current state-of-the-art on the development of antioxidant compounds incorporating the pyrazole pharmacophore. It is a well-timed review driven by the increasing number of papers, on this issue, that have been published since the beginning of the 21st century (from 2000 to 2017). The aim is to look deeper into the structures already published in the literature containing the pyrazole core as the unique pharmacophore or combined with other pharmacophores and see the relationship between the presence of this five-membered nitrogen heterocycle and the behaviour of the compounds as potential antioxidant agents. An attempt was made to whenever possible establish structure-activity relationships that could help the design of new and more potent antioxidant agents containing this important pharmacophore. [Display omitted] •Pyrazole is an important pharmacophore in the development of antioxidants.•Pyrazoles alone or combined with other pharmacophores showed high antioxidant activity.•Hybridization with known antioxidants can be a strategy to increase pyrazoles activity.•Important structure-activity relationships were disclosed and presented herein.