- 3-Aryl-4-(arylhydrazono)-1H-pyrazol-5-ones: Highly ligand efficient and potent inhibitors of GSK3β
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A series of 3-aryl-4-(arylhydrazono)-1H-pyrazol-5-one inhibitors of GSK3β was developed from a low molecular weight, highly ligand efficient screening hit 1. Hit-to-lead optimization led to a number of highly potent inhibitors, while maintaining the high ligand efficiency of the screening hit.
- Arnost, Michael,Pierce, Al,Haar, Ernst ter,Lauffer, David,Madden, Jaren,Tanner, Kirk,Green, Jeremy
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scheme or table
p. 1661 - 1664
(2010/07/03)
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- Method for preparing 2-pyrazolin-5-ones from 1,2,4-oxadiazoles
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A method for preparing 2-pyrazolin-5-ones from 1,2,4-oxadiazoles is described. The method comprises forming a liquid reaction system of a base catalyst and a 1,2,4-oxadiazole in an organic liquid reaction medium and heating the reaction system to a temperature sufficient to cause the 1,2,4-oxadiazole to be rearranged to a 2-pyrazolin-5-one.
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