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3,4,5-Trisubstituted isoxazoles as novel PPARdelta agonists: Part 1 |
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| Authors: | Epple Robert Russo Ross Azimioara Mihai Cow Christopher Xie Yongping Wang Xing Wityak John Karanewsky Don Gerken Andrea Iskandar Maya Saez Enrique Martin Seidel H Tian Shin-Shay |
| Institution: | Department of Medicinal Chemistry, The Genomics Institute of the Novartis Research Foundation, San Diego, CA 92121, USA. repple@gnf.org |
| Abstract: | We report the identification of a novel series of trisubstituted isoxazoles as PPAR activators from a high-throughput screen. A series of structural optimizations led to improved efficacy and excellent functional receptor selectivity for PPARdelta. The isoxazoles represent a series of agonists which display a scaffold that lies outside the typical PPAR agonist motif. |
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