Design, synthesis, and testing of potential antisickling agents. 7. Ethacrynic acid analogs

DJ Abraham, AS Mehanna, FS Williams…

文献索引：Abraham, D. J.; Mehanna, A. S.; Williams, F. S.; Cragoe, E. J.; Woltersdorf, O. W. Journal of Medicinal Chemistry, 1989 , vol. 32, # 11 p. 2460 - 2467

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被引用次数: 24

摘要

In search of a drug to treat sickle cell anemia, several analogues of the diuretic ethacrynic acid (ECA) have been synthesized and found equivalent in antigelling potency to ECA, but they have moderate or little diuretic activity. Structure-activity studies revealed that most of the highly active derivatives contain an acryloyl moiety. The latter functionality reacts covalently with protein sulfhydryl groups via a Michael addition reaction. Other derivatives, ...