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A novel series of non-carboxylic acid, non-hydantoin inhibitors of aldose reductase with potent oral activity in diabetic rat models: 6-(5-chloro-3-methylbenzofuran-2- …

…, DA Beebe, EL Conn, JB Coutcher…

文献索引:Mylari; Oates; Beebe; Brackett; Coutcher; Dina; Zembrowski Journal of Medicinal Chemistry, 2001 , vol. 44, # 17 p. 2695 - 2700

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被引用次数: 55

摘要

Discovery of a highly selective, potent, and safe non-carboxylic acid, non-hydantoin inhibitor of aldose reductase (AR) capable of potently blocking the excess glucose flux through the polyol pathway that prevails under diabetic conditions has been a long-standing challenge. In response, we did high-throughput screening of our internal libraries of compounds and identified 6-phenylsulfonylpyridazin-2 H-3-one, 8, which showed modest inhibition of AR, ...