Abstract
In an effort to develop safe and efficacious compounds for the treatment of metabolic disorders, novel thiophene substituted oxazole containing α-alkoxy-phenylpropanoic acid derivatives are designed as highly potent PPARα/γ dual agonists. These compounds were found to be efficacious at picomolar concentrations. Lead compound 18d has emerged as very potent PPARα/γ dual agonist demonstrating potent antidiabetic and lipid lowering activity at a very low dose and did not exhibit any significant signs of toxicity in rodents.
Copyright © 2011 Elsevier Ltd. All rights reserved.
MeSH terms
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Administration, Oral
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Animals
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Cell Line
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Dose-Response Relationship, Drug
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Hypoglycemic Agents / chemical synthesis
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Hypoglycemic Agents / chemistry
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Hypoglycemic Agents / pharmacology
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Inhibitory Concentration 50
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Mice
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Molecular Structure
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Oxazoles / chemistry
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PPAR alpha / agonists*
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PPAR gamma / agonists*
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Phenylpropionates / chemical synthesis*
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Phenylpropionates / chemistry
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Phenylpropionates / pharmacology*
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Protein Binding / drug effects
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Rats
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Rats, Wistar
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Rosiglitazone
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Thiazolidinediones / chemical synthesis
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Thiazolidinediones / chemistry
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Thiazolidinediones / pharmacology
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Thiophenes / chemistry
Substances
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Hypoglycemic Agents
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Oxazoles
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PPAR alpha
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PPAR gamma
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Phenylpropionates
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Thiazolidinediones
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Thiophenes
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Rosiglitazone