Design and Synthesis of Dual Peroxisome Proliferator-Activated Receptors and 
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- 作者：Yanping Xu ; Garret J. Etgen ; Carol L. Broderick ; Emily Canada ; Isabel Gonzalez ; Jason Lamar ; Chahrzad Montrose-Rafizadeh ; Brian A. Oldham ; John J. Osborne ; Chaoyu Xie ; Qing Shi ; Leonard L. Winneroski
- 刊名：Journal of Medicinal Chemistry
- 出版年：2006
- 出版时间：September 21, 2006
- 年：2006
- 卷：49
- 期：19
- 页码：5649 - 5652
- 全文大小：80K
- 年卷期：v.49,no.19(September 21, 2006)
- ISSN：1520-4804
文摘
The design and synthesis of the dual peroxisome proliferator-activated receptor (PPAR) 
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agonist (R)-3-{4-[3-(4-chloro-2-phenoxy-phenoxy)-butoxy]-2-ethyl-phenyl}-propionic acid (20) for the treatmentof type 2 diabetes and associated dyslipidemia is described. Thecompound possesses a potent dual hPPAR / agonist profile (IC50 =19 nM/4 nM; EC50 = 102 nM/6 nM for hPPAR and hPPAR,respectively). In preclinical models, the compound improves insulinsensitivity and reverses diabetic hyperglycemia with less weight gainat a given level of glucose control relative to rosiglitazone.
/ agonist (R)-3-{4-[3-(4-chloro-2-phenoxy-phenoxy)-butoxy]-2-ethyl-phenyl}-propionic acid (20) for the treatmentof type 2 diabetes and associated dyslipidemia is described. Thecompound possesses a potent dual hPPAR / agonist profile (IC50 =19 nM/4 nM; EC50 = 102 nM/6 nM for hPPAR and hPPAR,respectively). In preclinical models, the compound improves insulinsensitivity and reverses diabetic hyperglycemia with less weight gainat a given level of glucose control relative to rosiglitazone.