(-)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 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.
Lohray
B B
BB
Discovery Synthesis and Discovery Biology, Dr. Reddy's Research Foundation, 7-1-27, Ameerpet, Hyderabad 500 016, India.
Lohray
V B
VB
Bajji
A C
AC
Kalchar
S
S
Poondra
R R
RR
Padakanti
S
S
Chakrabarti
R
R
Vikramadithyan
R K
RK
Misra
P
P
Juluri
S
S
Mamidi
N V
NV
Rajagopalan
R
R
D000818:Animals; D001682:Biological Availability; D001786:Blood Glucose / Q000032:analysis*; D048909:Diabetes Complications; D003920:Diabetes Mellitus / Q000188:drug therapy; D006949:Hyperlipidemias / Q000150:complications / Q000188:drug therapy; D007004:Hypoglycemic Agents / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D007333:Insulin Resistance; D051379:Mice; D010078:Oxazines / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D010666:Phenylpropionates / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D051381:Rats; D017208:Rats, Wistar; D018160:Receptors, Cytoplasmic and Nuclear / Q000819:agonists*; D013237:Stereoisomerism; D014157:Transcription Factors / Q000819:agonists*; D014280:Triglycerides / Q000097:blood*
D001786:Blood Glucose; D007004:Hypoglycemic Agents; D010078:Oxazines; D010666:Phenylpropionates; D018160:Receptors, Cytoplasmic and Nuclear; D014157:Transcription Factors; D014280:Triglycerides; C432703:ragaglitazar