1. Identification of 5-arylidene-4-thiazolidinone derivatives endowed with dual activity as aldose reductase inhibitors and antioxidant agents for the treatment of diabetic complications
- Author
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Mario Cappiello, Umberto Mura, Ettore Novellino, Federico Da Settimo, Stefania Sartini, Sandro Cosconati, Rosanna Maccari, Rosaria Ottanà, Luciana Marinelli, Concettina La Motta, Marco Giglio, Antonella Del Corso, Ottana, R, Maccari, R, Giglio, M, Del Corso, A, Cappiello, M, Mura, U, Cosconati, Sandro, Marinelli, L, Novellino, E, Sartini, S, La Motta, C, Da Settimo, F., Rosaria, Ottan, Rosanna, Maccari, Marco, Giglio, Antonella Del, Corso, Mario, Cappiello, Umberto, Mura, Sandro, Cosconati, Marinelli, Luciana, Novellino, Ettore, Stefania, Sartini, Concettina La, Motta, and Federico Da, Settimo
- Subjects
Diabetes mellitu ,Antioxidant ,Antioxidant agent ,medicine.medical_treatment ,Aldose reductase ,Acetates ,medicine.disease_cause ,Antioxidants ,Diabetes Complications ,Structure-Activity Relationship ,Diabetes mellitus ,Aldehyde Reductase ,5-arylidene-4-thiazolidinones ,Molecular docking ,Drug Discovery ,5-arylidene-4- thiazolidinone ,medicine ,Structure–activity relationship ,Animals ,Humans ,Enzyme Inhibitors ,Pharmacology ,chemistry.chemical_classification ,biology ,Organic Chemistry ,General Medicine ,medicine.disease ,Molecular Docking Simulation ,Oxidative Stress ,Enzyme ,chemistry ,Biochemistry ,Enzyme inhibitor ,biology.protein ,Cattle ,Thiazolidinediones ,Oxidative stress - 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. © 2011 Elsevier Masson SAS. All rights reserved.
- Published
- 2011