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2-Alkoxydihydrocinnamates as PPAR agonists. Activity modulation by the incorporation of phenoxy substituents |
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| Authors: | 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 |
| Affiliation: | Lilly Research Laboratories, Division of Eli Lilly & Company, Lilly S.A., Alcobendas 28108, Madrid, Spain. martin_jose_alfredo@lilly.com |
| Abstract: | Herein we describe a series of potent and selective PPARgamma agonists with moderate PPARalpha 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. |
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