（-）3-[4-[2-（吩恶嗪-10-基）乙氧基]苯基]-2-乙氧基丙酸[（-）DRF 2725]：一种具有强效抗高血糖和脂质调节活性的双重过氧化物酶体增殖物激活受体激动剂。
(-)3-[4-[2-(Phenoxazin-10-yl)ethoxy]phenyl]-2-ethoxypropanoic acid [(-)DRF 2725]: a dual PPAR agonist with potent antihyperglycemic and lipid modulating activity.
作者信息
Lohray B B, Lohray V B, Bajji A C, Kalchar S, Poondra R R, Padakanti S, Chakrabarti R, Vikramadithyan R K, Misra P, Juluri S, Mamidi N V, Rajagopalan R
机构信息
Discovery Synthesis and Discovery Biology, Dr. Reddy's Research Foundation, 7-1-27, Ameerpet, Hyderabad 500 016, India.
出版信息
J Med Chem. 2001 Aug 2;44(16):2675-8. doi: 10.1021/jm010143b.
(-)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.
（-）DRF 2725（6）是苯丙酸的吩恶嗪类似物。化合物6显示出有趣的过氧化物酶体增殖物激活受体α（PPARα）和过氧化物酶体增殖物激活受体γ（PPARγ）双重激活作用。在胰岛素抵抗的db/db小鼠中，与罗格列酮相比，化合物6能更好地降低血糖和甘油三酯水平。化合物6还显示出良好的口服生物利用度和令人印象深刻的药代动力学特征。我们的研究表明，化合物6作为治疗糖尿病和血脂异常的药物具有巨大潜力。
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