Abstract
Inhibition of the PHD2 enzyme has been associated with increased red blood cell levels. From a screening hit, a series of novel hydroxyl-thiazoles were developed as potent PHD2 inhibitors.
MeSH terms
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Chemistry, Pharmaceutical / methods
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Diabetes Mellitus / drug therapy
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Drug Design
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Drug Evaluation, Preclinical / methods
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Erythrocytes / enzymology
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Humans
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Hypoxia-Inducible Factor 1, alpha Subunit / chemical synthesis*
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Hypoxia-Inducible Factor 1, alpha Subunit / chemistry
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Inhibitory Concentration 50
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Models, Chemical
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Models, Molecular
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Myocardial Infarction / drug therapy
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Peripheral Vascular Diseases / therapy
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Stroke / drug therapy
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Structure-Activity Relationship
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Thiazoles / chemistry*
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Thiazoles / pharmacology
Substances
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Hypoxia-Inducible Factor 1, alpha Subunit
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Thiazoles