Thiazolidine-2, 4-dione derivatives having one or two substituent (s) such as phenyl, heteryl and alkyl group (s) at the 5-position were synthesized and evaluated as aldose reductase inhibitors. Inhibition by the active compounds of the swelling of the lens in a rat-lens-culture assay was also measured. Among these compounds, a series of 5-(3, 4-dialkoxyphenyl) thiazolidine-2, 4-diones showed pronounced activities in both assays. Structure-activity relationships are discussed and a new approach to the synthesis of 5-arylthiazolidine-2, 4-diones is described.
具有一个或两个取代基(如苯基、杂基和烷基)的
噻唑烷-2,4-二酮衍
生物在5位合成并评估为醛糖还原酶
抑制剂。在鼠晶状体培养检测中,活性化合物的抑制作用也被测量。在这些化合物中,一系列5-(3,4-二烷氧基苯基)
噻唑烷-2,4-二酮在两种检测中显示出显著的活性。结构-活性关系进行了讨论,并描述了一种合成5-芳基
噻唑烷-2,4-二酮的新方法。