477982-30-2Relevant academic research and scientific papers
An asymmetric synthesis of PPAR-γ agonist navaglitazar from (+)-methyl (2S,3R)-3-(4-methoxyphenyl)glycidate
Rizzo, John R.,Zhang, Tony Y.
, p. 580 - 583 (2007/10/03)
An asymmetric synthesis of navaglitazar, a peroxisome proliferator activated receptor (PPAR) γ agonist, from commercially available (+)-methyl (2S,3R)-3-(4-methoxyphenyl)glycidate, is described. The new synthesis features high overall yield, low solvent usage, crystalline intermediates and operational simplicity. Schweizerische Chemische Gesellschaft.
2-Alkoxydihydrocinnamates as PPAR agonists. Activity modulation by the incorporation of phenoxy substituents
Martín, José A.,Brooks, Dawn A.,Prieto, Lourdes,González, Rosario,Torrado, Alicia,Rojo, Isabel,López De Uralde, Beatriz,Lamas, Carlos,Ferritto, Rafael,Dolores Martín-Ortega, María,Agejas, Javier,Parra, Francisco,Rizzo, John R.,Rhodes, Gary A.,Robey, Roger L.,Alt, Charles A.,Wendel, Samuel R.,Zhang, Tony Y.,Reifel-Miller, Anne,Montrose-Rafizadeh, Chahrzad,Brozinick, Joseph T.,Hawkins, Eric,Misener, Elizabeth A.,Briere, Daniel A.,Ardecky, Robert,Fraser, James D.,Warshawsky, Alan M.
, p. 51 - 55 (2007/10/03)
Herein we describe a series of potent and selective PPARγ agonists with moderate PPARα affinity and little to no affinity for other nuclear receptors. In vivo studies in a NIDDM animal model (ZDF rat) showed that these compounds are efficacious at low doses in glucose normalization and plasma triglyceride reduction. Compound 1b (LY519818) was selected from our SAR studies to be advanced to clinical evaluation for the treatment of type II diabetes. Herein we describe a series of potent and selective PPARγ agonists with moderate PPARα affinity and little to no affinity for other nuclear receptors. In vivo studies in a NIDDM animal model (ZDF rat) showed that these compounds are efficacious at low doses in glucose normalization and plasma triglyceride reduction. Compound 1b (LY519818) was selected from our SAR studies to be advanced to clinical evaluation for the treatment of type II diabetes.
