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1. (-)3-[4-[2-(Phenoxazin-10-yl)ethoxy]phenyl]-2-ethoxypropanoic acid [(-)DRF 2725]: a dual PPAR agonist with potent antihyperglycemic and lipid modulating activity.

Author

Lohray BB, Lohray VB, Bajji AC, Kalchar S, Poondra RR, Padakanti S, Chakrabarti R, Vikramadithyan RK, Misra P, Juluri S, Mamidi NV, and Rajagopalan R

Subjects
Animals, Biological Availability, Diabetes Complications, Diabetes Mellitus drug therapy, Hyperlipidemias complications, Hyperlipidemias drug therapy, Hypoglycemic Agents pharmacokinetics, Hypoglycemic Agents pharmacology, Insulin Resistance, Mice, Oxazines pharmacokinetics, Oxazines pharmacology, Phenylpropionates pharmacokinetics, Phenylpropionates pharmacology, Rats, Rats, Wistar, Stereoisomerism, Blood Glucose analysis, Hypoglycemic Agents chemical synthesis, Oxazines chemical synthesis, Phenylpropionates chemical synthesis, Receptors, Cytoplasmic and Nuclear agonists, Transcription Factors agonists, Triglycerides blood
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.

Published
2001
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