Journal of medicinal chemistry

Inhibition of glyoxalase I: the first low-nanomolar tight-binding inhibitors

SS More, R Vince

文献索引：More, Swati S.; Vince, Robert Journal of Medicinal Chemistry, 2009 , vol. 52, # 15 p. 4650 - 4656

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被引用次数: 38

摘要

A series of rational modifications to the structure of known S-(N-aryl-N-hydroxycarbamoyl) glutathione-based glyoxalase I inhibitors culminated in the discovery of the first single-digit nanomolar inhibitor. This study makes available key information about possible means to address the issues of metabolic instability, low potency, and synthetic complexicity that have plagued the area of glyoxalase I inhibition. Knowledge garnered from this study has ...