Journal
MOLECULES
Volume 27, Issue 8, Pages -Publisher
MDPI
DOI: 10.3390/molecules27082599
Keywords
quinazolin-4(3H)-one; phenol derivatives; antioxidant; hybrid molecules; in vitro evaluation
Funding
- Iuliu Hatieganu University of Medicine and Pharmacy, Cluj-Napoca, Romania [PCD 2461/54/17.01.2020, 1033/50/13.01.2021]
- Romanian Ministry of Research and Innovation [PN 19 35 02 01]
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Considering the damage caused by ROS and RNS in the human body, finding new therapeutic agents with superior efficacy is crucial. Four series of new hybrid molecules were synthesized and evaluated for their antioxidant potential. Some compounds showed stronger antioxidant effects.
Considering the important damage caused by the reactive oxygen (ROS) and nitrogen (RNS) species in the human organism, the need for new therapeutic agents, with superior efficacy to the known natural and synthetic antioxidants, is crucial. Quinazolin-4-ones are known for their wide range of biological activities, and phenolic compounds display an important antioxidant effect. Linking the two active pharmacophores may lead to an increase of the antioxidant activity. Therefore, we synthesized four series of new hybrid molecules bearing the quinazolin-4-one and phenol scaffolds. Their antioxidant potential was evaluated in vitro, considering different possible mechanisms of action: hydrogen atom transfer, ability to donate electrons and metal ions chelation. Theoretical quantum and thermodynamical calculations were also performed. Some compounds, especially the ortho diphenolic ones, exerted a stronger antioxidant effect than ascorbic acid and Trolox.
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