An investigation on 4-thiazolidinone derivatives as dual inhibitors of aldose reductase and protein tyrosine phosphatase 1B, in the search for potential agents for the treatment of type 2 diabetes mellitus and its complications

[Display omitted] •4-Thiazolidinones were synthesised and tested as dual AR/PTP1B inhibitors.•SAR, molecular docking and kinetic studies were carried out.•Two compounds endowed with interesting AR/PTP1B inhibition profiles were identified.•Features useful to achieve simultaneous inhibition of both A...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2018-12, Vol.28 (23-24), p.3712-3720
Hauptverfasser:	Maccari, Rosanna, Del Corso, Antonella, Paoli, Paolo, Adornato, Ilenia, Lori, Giulia, Balestri, Francesco, Cappiello, Mario, Naß, Alexandra, Wolber, Gerhard, Ottanà, Rosaria
Format:	Artikel
Sprache:	eng
Schlagworte:	4-Thiazolidinone derivatives Aldehyde Reductase - antagonists & inhibitors Aldehyde Reductase - metabolism Aldose reductase Designed multiple ligands Diabetes mellitus Diabetes Mellitus, Type 2 - drug therapy Diabetes Mellitus, Type 2 - metabolism Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology Humans Hypoglycemic Agents - chemistry Hypoglycemic Agents - pharmacology Ligands Molecular Docking Simulation Protein tyrosine phosphatase 1B Protein Tyrosine Phosphatase, Non-Receptor Type 1 - antagonists & inhibitors Protein Tyrosine Phosphatase, Non-Receptor Type 1 - metabolism Structure-Activity Relationship Thiazolidines - chemistry Thiazolidines - pharmacology
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