Abstract
A series of 3-anilino-quinoxalinones has been identified as a new class of glycogen phosphorylase inhibitors. The lead compound 1 was identified through high throughput screening as well as through pharmacophore-based electronic screening. Modifications were made to the scaffold of 1 to produce novel analogues, some of which are 25 times more potent than the lead compound.
MeSH terms
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Animals
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Blood Glucose / drug effects
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Drug Evaluation, Preclinical
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Enzyme Inhibitors / chemical synthesis
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Enzyme Inhibitors / pharmacokinetics
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Glycogen Phosphorylase / antagonists & inhibitors*
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Hypoglycemic Agents / chemical synthesis*
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Hypoglycemic Agents / pharmacokinetics
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Inhibitory Concentration 50
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Mice
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Mice, Obese
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Quinoxalines
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Structure-Activity Relationship
Substances
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Blood Glucose
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Enzyme Inhibitors
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Hypoglycemic Agents
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Quinoxalines
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Glycogen Phosphorylase