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Identification of 5-arylidene-4-thiazolidinone derivatives endowed with dual activity as aldose reductase inhibitors and antioxidant agents for the treatment of diabetic complications |
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| Authors: | Ottanà Rosaria Maccari Rosanna Giglio Marco Del Corso Antonella Cappiello Mario Mura Umberto Cosconati Sandro Marinelli Luciana Novellino Ettore Sartini Stefania La Motta Concettina Da Settimo Federico |
| Affiliation: | a Dipartimento Farmaco-chimico, Università di Messina, Polo Universitario Annunziata, 98168 Messina, Italy b Dipartimento di Biologia, Unità di Biochimica, Università di Pisa, Via S. Zeno 51, 56127 Pisa, Italy c Dipartimento di Chimica Farmaceutica e Tossicologica, Università di Napoli “Federico II”, Via D. Montesano 49, 80131 Napoli, Italy d Dipartimento di Scienze Farmaceutiche, Università di Pisa, Via Bonanno 6, 56126 Pisa, Italy |
| Abstract: | In continuing the search for more effective 5-arylidene-4-thiazolidinones as aldose reductase inhibitors, a new set of suitably substituted compounds (4, 5 and 8) was explored. Acetic acids 5, particularly 5a and 5h, proved to be interesting inhibitors of the enzyme as well as excellent antioxidant agents that are potentially able to counteract the oxidative stress associated with both diabetic complications as well as other pathologies. Molecular docking experiments supported SAR studies. |
| Keywords: | Diabetes mellitus Aldose reductase Antioxidant agent 5-arylidene-4-thiazolidinones Molecular docking |
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