Synthesis and aldose reductase inhibitory activity of 5-arylidene-2, 4-thiazolidinediones

…, L Costantino, C Curinga, R Maccari, F Monforte…

文献索引：Bruno; Costantino; Curinga; Maccari; Monforte; Nicolo; Ottana; Vigorita Bioorganic and Medicinal Chemistry, 2002 , vol. 10, # 4 p. 1077 - 1084

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被引用次数: 164

摘要

Several (Z)-5-arylidene-2, 4-thiazolidinediones were synthesized and tested as aldose reductase inhibitors (ARIs). The most active of the N-unsubstituted derivatives (2) exerted the same inhibitory activity of Sorbinil. The introduction of an acetic side chain on N-3 of the thiazolidinedione moiety led to a marked increase in lending inhibitory activity, conducting to the discovery of a very potent ARI (4c), whose activity level (IC50= 0.13 μM) was in the ...