(−)3-[4-[2-(Phenoxazin-10-yl)ethoxy]phenyl]-2-ethoxypropanoic Acid [(−)DRF 2725]: A Dual PPAR Agonist with Potent Antihyperglycemic and Lipid Modulating Activity

(−)DRF 2725 (6) is a phenoxazine analogue of phenyl propanoic acid. Compound 6 showed interesting dual activation of PPARα and PPARγ. 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...

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Veröffentlicht in:	Journal of medicinal chemistry 2001-08, Vol.44 (16), p.2675-2678
Hauptverfasser:	Lohray, Braj B, Lohray, Vidya B, Bajji, Ashok C, Kalchar, Shivaramayya, Poondra, Rajamohan R, Padakanti, Srinivas, Chakrabarti, Ranjan, Vikramadithyan, Reeba K, Misra, Parimal, Juluri, Suresh, Mamidi, N. V. S. Rao, Rajagopalan, Ramanujam
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Biological and medical sciences Biological Availability Blood Glucose - analysis Diabetes Complications Diabetes Mellitus - drug therapy General and cellular metabolism. Vitamins Hyperlipidemias - complications Hyperlipidemias - drug therapy Hypoglycemic Agents - chemical synthesis Hypoglycemic Agents - pharmacokinetics Hypoglycemic Agents - pharmacology Insulin Resistance Medical sciences Mice Oxazines - chemical synthesis Oxazines - pharmacokinetics Oxazines - pharmacology Pharmacology. Drug treatments Phenylpropionates - chemical synthesis Phenylpropionates - pharmacokinetics Phenylpropionates - pharmacology Rats Rats, Wistar Receptors, Cytoplasmic and Nuclear - agonists Stereoisomerism Transcription Factors - agonists Triglycerides - blood
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Zusammenfassung:	(−)DRF 2725 (6) is a phenoxazine analogue of phenyl propanoic acid. Compound 6 showed interesting dual activation of PPARα and PPARγ. 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.
ISSN:	0022-2623 1520-4804
DOI:	10.1021/jm010143b