Discovery of benzothiazole-based thiazolidinones as potential anti-inflammatory agents: anti-inflammatory activity, soybean lipoxygenase inhibition effect and molecular docking studies.
| Autor: | Haroun M; Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa, Saudi Arabia., Petrou A; School of Pharmacy, Aristotle University of Thessaloniki, Thessaloniki, Greece., Tratrat C; Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa, Saudi Arabia., Kositsi K; School of Pharmacy, Aristotle University of Thessaloniki, Thessaloniki, Greece., Gavalas A; School of Pharmacy, Aristotle University of Thessaloniki, Thessaloniki, Greece., Geronikaki A; School of Pharmacy, Aristotle University of Thessaloniki, Thessaloniki, Greece., Venugopala KN; Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa, Saudi Arabia.; Department of Biotechnology and Food Technology, Faculty of Applied Sciences, Durban University of Technology, Durban, South Africa., Harsha NS; Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa, Saudi Arabia.; Department of Pharmaceutics, Vidya Siri College of Pharmacy, Bangalore, India. |
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| Jazyk: | angličtina |
| Zdroj: | SAR and QSAR in environmental research [SAR QSAR Environ Res] 2022 Jun; Vol. 33 (6), pp. 485-497. |
| DOI: | 10.1080/1062936X.2022.2084772 |
| Abstrakt: | Despite the greatest achievement in the development of anti-inflammatory agents in the last two decades, the current clinical drugs suffer from a variety of complications in community settings and hospital. There is still an urgent need to design novel molecules with better safety profile and with different molecular targets from those in current clinical use. The aim of this research was to discover a series of benzothiazole-based thiazolidinones with lipoxygenase (LOX) inhibitory activity as a mechanism of anti-inflammatory action. Carrageenan-induced mouse foot paw oedema assay was carried out to determine the anti-inflammatory activity, while LOX inhibition was examined through the conversion of sodium linoleate to 13-hydroperoxylinoleic acid. Molecular docking studies were performed using AutoDock 4.2 software. The anti-inflammatory activity of the title compounds was determined in a range of 18.4%-69.57%, where compound #3 was found to be the most potent (69.57%) and also to be more active than the reference drug indomethacin (47%). Moreover, compound #3 showed the highest LOX inhibitory activity with IC |
| Databáze: | MEDLINE |
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