Abstract
A series of indazoles have been discovered as KHK inhibitors from a pyrazole hit identified through fragment-based drug discovery (FBDD). The optimization process guided by both X-ray crystallography and solution activity resulted in lead-like compounds with good pharmaceutical properties.
Copyright © 2011 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Crystallography, X-Ray
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Dose-Response Relationship, Drug
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Drug Discovery*
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Fructokinases / antagonists & inhibitors*
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Indazoles / chemical synthesis
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Indazoles / chemistry
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Indazoles / pharmacology*
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Models, Molecular
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Molecular Structure
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Pyrazoles / chemistry*
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Stereoisomerism
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Structure-Activity Relationship
Substances
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Indazoles
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Pyrazoles
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pyrazole
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Fructokinases
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ketohexokinase