Article

3,4,5-Trisubstituted isoxazoles as novel PPARdelta agonists: Part 1.

Department of Medicinal Chemistry, The Genomics Institute of the Novartis Research Foundation, San Diego, CA 92121, USA.
Bioorganic & Medicinal Chemistry Letters (impact factor: 2.55). 09/2006; 16(16):4376-80. DOI:10.1016/j.bmcl.2006.05.055
Source: PubMed

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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    TheScientificWorldJOURNAL 02/2006; 6:1770-82. · 1.66 Impact Factor
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Keywords

agonists
 
excellent functional receptor selectivity
 
high-throughput screen
 
novel series
 
PPAR activators
 
PPARdelta
 
structural optimizations
 
typical PPAR agonist motif