Abstract
3-Aryl-5-phenyl-(1,2,4)-triazoles were identified as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1). They are active in both in vitro and an in vivo mouse pharmacodynamic (PD) model. The synthesis and structure activity relationships are presented.
MeSH terms
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11-beta-Hydroxysteroid Dehydrogenase Type 1 / antagonists & inhibitors*
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Animals
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Binding Sites
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Disease Models, Animal
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Enzyme Inhibitors* / chemical synthesis
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Enzyme Inhibitors* / pharmacokinetics
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Enzyme Inhibitors* / therapeutic use
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Hydrocarbons, Aromatic* / chemical synthesis
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Hydrocarbons, Aromatic* / pharmacology
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Hydrocarbons, Aromatic* / therapeutic use
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Hypoglycemic Agents* / chemical synthesis
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Hypoglycemic Agents* / pharmacokinetics
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Hypoglycemic Agents* / therapeutic use
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Inhibitory Concentration 50
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Metabolic Syndrome / drug therapy*
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Mice
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Models, Chemical
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Structure-Activity Relationship
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Triazoles* / chemical synthesis
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Triazoles* / pharmacology
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Triazoles* / therapeutic use
Substances
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Enzyme Inhibitors
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Hydrocarbons, Aromatic
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Hypoglycemic Agents
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Triazoles
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11-beta-Hydroxysteroid Dehydrogenase Type 1