Optimization of a pyrazole hit from FBDD into a novel series of indazoles as ketohexokinase inhibitors.
Bioorganic & Medicinal Chemistry Letters(2011)
摘要
A series of indazoles have been discovered as KHK inhibitors from a pyrazole hit identified through fragment based drug discovery. The lead compounds showed KHK enzyme activity in the nM range with amendable pharmaceutical properties.
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关键词
FBDD (fragment based drug discovery),KHK (ketohexokinase),Pyrazole,Indazole
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