Abstract
(-)DRF 2725 (6) is a phenoxazine analogue of phenyl propanoic acid. Compound 6 showed interesting dual activation of PPAR alpha and PPAR gamma. In insulin resistant db/db mice, 6 showed better reduction of plasma glucose and triglyceride levels as compared to rosiglitazone. Compound 6 has also shown good oral bioavailability and impressive pharmacokinetic characteristics. Our study indicates that 6 has great potential as a drug for diabetes and dyslipidemia.
MeSH terms
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Animals
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Biological Availability
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Blood Glucose / analysis*
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Diabetes Complications
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Diabetes Mellitus / drug therapy
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Hyperlipidemias / complications
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Hyperlipidemias / drug therapy
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Hypoglycemic Agents / chemical synthesis*
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Hypoglycemic Agents / pharmacokinetics
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Hypoglycemic Agents / pharmacology
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Insulin Resistance
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Mice
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Oxazines / chemical synthesis*
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Oxazines / pharmacokinetics
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Oxazines / pharmacology
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Phenylpropionates / chemical synthesis*
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Phenylpropionates / pharmacokinetics
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Phenylpropionates / pharmacology
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Rats
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Rats, Wistar
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Receptors, Cytoplasmic and Nuclear / agonists*
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Stereoisomerism
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Transcription Factors / agonists*
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Triglycerides / blood*
Substances
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Blood Glucose
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Hypoglycemic Agents
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Oxazines
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Phenylpropionates
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Receptors, Cytoplasmic and Nuclear
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Transcription Factors
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Triglycerides
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ragaglitazar