| Literature DB >> 15582409 |
José A Martín1, Dawn A Brooks, Lourdes Prieto, Rosario González, Alicia Torrado, Isabel Rojo, Beatriz López de Uralde, Carlos Lamas, Rafael Ferritto, María Dolores Martín-Ortega, Javier Agejas, Francisco Parra, John R Rizzo, Gary A Rhodes, Roger L Robey, Charles A Alt, Samuel R Wendel, Tony Y Zhang, Anne Reifel-Miller, Chahrzad Montrose-Rafizadeh, Joseph T Brozinick, Eric Hawkins, Elizabeth A Misener, Daniel A Briere, Robert Ardecky, James D Fraser, Alan M Warshawsky.
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.Entities:
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Year: 2005 PMID： 15582409 DOI： 10.1016/j.bmcl.2004.10.042
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823