What is it about?

Sulfonamide-based drugs are most of the sulfur-containing drugs approved by the United States Food and Drug Administration (FDA). Although sulfonamide derivatives have been extensively exploited as antibacterial agents, their therapeutic potential as antioxidants is relatively underexplored despite the prevalence of oxidative stress-mediated diseases and the urgent need for new and more effective antioxidant drugs. Several sulfonamide derivatives exhibit significant antioxidant activities in terms of radical scavenging. Also many were shown to activate the nuclear factor erythroid 2-related factor 2 (Nrf2), the main regulator of the endogenous antioxidant response, a critical process used by cells in response to oxidative stress. The antioxidant role of sulfonamides and derivatives as Nrf2 activators is also reviewed. The antioxidant mechanism of action of sulfonamides has not been fully clarified, but as they have antioxidant properties, it is a subject worthy of in-depth study. The present review is focused on sulfonamides and derivatives as potential antioxidants along the period 2013-2021 and intends to stimulate research in the are

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Why is it important?

This review aimed to perform an update on the antioxidant properties of selected sulfonamide derivatives with the view to stimulate research in the area and promote drug discovery programs based on this scaffold to find new lead compounds that can be valid assets for antioxidant therapy, namely against oxidative stress-mediated diseases such as diabetics, Parkinson’s disease, Alzheimer’s disease, Huntington’s disease, and cancer. The literature search revealed that about 90% of the reported sulfonamide derivatives displayed higher antioxidant activity than standard and commercially available antioxidant drugs, while about 10% exhibited comparable antioxidant activity

Perspectives

As sulfonamide-based derivatives possess a huge potential therapeutic value as antioxidants, additional structure-activity relationships and in silico studies are recommended to optimize their full potential. Moreover, sulfonamide derivatives are potential nuclear factor erythroid 2-related factor 2 (Nrf2) activators and, therefore, can positively regulate antioxidant genes and proteins.

Dr. Melford Chuka Egbujor
Federal University Otuoke

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This page is a summary of: Sulfonamide a Valid Scaffold for Antioxidant Drug Development, Mini-Reviews in Organic Chemistry, March 2023, Bentham Science Publishers,
DOI: 10.2174/1570193x19666220411134006.
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