In vitro aldose reductase inhibitory activity of 5-benzyl-2, 4-thiazolidinediones

D Rakowitz, R Maccari, R Ottanà, MG Vigorita

Index: Rakowitz, Dietmar; Maccari, Rosanna; Ottana, Rosaria; Vigorita, Maria Gabriella Bioorganic and Medicinal Chemistry, 2006 , vol. 14, # 2 p. 567 - 574

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Citation Number: 50

Abstract

Several 5-benzyl-2, 4-thiazolidinediones (5–7) were synthesised and tested as in vitro aldose reductase (ALR2) inhibitors. Most of them, particularly N-unsubstituted 5-benzyl-2, 4- thiazolidinediones 5 and (5-benzyl-2, 4-dioxothiazolidin-3-yl) acetic acids 7, displayed moderate to high inhibitory activity levels. In detail, the insertion of an acetic chain on N-3 significantly enhanced ALR2 inhibitory potency, leading to acids 7 which proved to be the ...