title: Identification of 5-arylidene-4-thiazolidinone derivatives endowed with dual activity as aldose reductase inhibitors and antioxidant agents for the treatment of diabetic complications.
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.
authors.affiliation: Dipartimento Farmaco-chimico, Università di Messina, Polo Universitario Annunziata, 98168 Messina, Italy. ottana@pharma.unime.it
authors.forename: Rosaria
authors.initials: R
authors.lastname: Ottanà
authors.forename: Rosanna
authors.initials: R
authors.lastname: Maccari
authors.forename: Marco
authors.initials: M
authors.lastname: Giglio
authors.forename: Antonella
authors.initials: A
authors.lastname: Del Corso
authors.forename: Mario
authors.initials: M
authors.lastname: Cappiello
authors.forename: Umberto
authors.initials: U
authors.lastname: Mura
authors.forename: Sandro
authors.initials: S
authors.lastname: Cosconati
authors.forename: Luciana
authors.initials: L
authors.lastname: Marinelli
authors.forename: Ettore
authors.initials: E
authors.lastname: Novellino
authors.forename: Stefania
authors.initials: S
authors.lastname: Sartini
authors.forename: Concettina
authors.initials: C
authors.lastname: La Motta
authors.forename: Federico
authors.initials: F
authors.lastname: Da Settimo
mesh_terms: D000085:Acetates / Q000737:chemistry; D000449:Aldehyde Reductase / Q000037:antagonists & inhibitors* / Q000737:chemistry; D000818:Animals; D000975:Antioxidants / Q000138:chemical synthesis* / Q000494:pharmacology; D002417:Cattle; D048909:Diabetes Complications / Q000517:prevention & control; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D062105:Molecular Docking Simulation; D018384:Oxidative Stress / Q000187:drug effects; D013329:Structure-Activity Relationship; D045162:Thiazolidinediones / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D000085:Acetates; D000975:Antioxidants; D004791:Enzyme Inhibitors; D045162:Thiazolidinediones; D000449:Aldehyde Reductase