AI Article Synopsis
- Myeloperoxidase (MPO) is crucial for human immunity by producing hypochlorous acid to combat microorganisms, but it can also damage tissues when released outside phagocytes.
- MPO is linked to various inflammatory diseases, making it a promising target for new therapies.
- This study developed and tested isomeric 1,3-dihydro-2H-benzo[d]imidazole-2-thione derivatives, identifying 2-(2-thioxo-2,3-dihydro-1H-benzo[d]imidazole-1-yl)acetohydrazide (C19) as the most potent inhibitor of MPO activity.
Article Abstract
Myeloperoxidase (MPO) plays a key role in human antimicrobial system by oxidizing vital molecules of microorganisms in phagolysosomes through produced hypochlorous acid (HOCl). However, MPO can be released outside the phagocyte and produces reactive intermediates leading to tissue damage. MPO, as a local mediator of tissue damage, has been associated with inflammatory diseases such as renal injury, multiple sclerosis, cardiovascular and neurodegenerative diseases. Therefore, the enzyme currently draws attention as a potential therapeutic target. In this study, isomeric 1,3-dihydro-2H-benzo[d]imidazole-2-thione derivatives having amide, hydrazide and hydroxamic acid groups either on nitrogen or on sulphur atom were designed and their inhibitory activity was determined on chlorination and peroxidation cycles of MPO. Among the compounds, 2-(2-thioxo-2,3-dihydro-1H-benzo[d]imidazole-1-yl)acetohydrazide(C19) was found as the most active inhibitor on both cycles.
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| http://dx.doi.org/10.1016/j.ejmech.2022.115083 | DOI Listing |
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