Biological activities and quantitative structure-activity relationships of spiro [imidazolidine-4, 4'(1'H)-quinazoline]-2, 2', 5 (3'H)-triones as aldose reductase inhibitors

M Yamagishi, Y Yamada, K Ozaki, M Asao…

文献索引：Yamagishi; Yamada; Ozaki; Asao; Shimizu; Suzuki; Matsumoto; Matsuoka Journal of Medicinal Chemistry, 1992 , vol. 35, # 11 p. 2085 - 2094

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被引用次数: 36

摘要

A series of spiro [imidazolidine-4, 4'(l'H)-q~ line]-2, 2', 5 (3'H)-triones were prepared and tested for aldose reductase inhibitory activity. The 6'-halogenated derivatives were found to be highly potent in vitro inhibitors of male rabbit lens aldose reductase and in vivo inhibitors of poly01 accumulation in the sciatic nerves of galactosemic rats. Of these,(4R)-6'-chloro-3'- methylspiro [imidazolidine-4, 4'(l'H)-quinazoline]-2, 2', 5 (3'H)-trione (67) showed the most ...