3,4,5-trisubstituted isoxazoles as novel PPAR delta agonists. Part 1

Academic Article

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• Research
• Identity
• Additional Document Info
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Overview

authors

• Epple, R.
• Russo, R.
• Azimioara, M.
• Cow, C.
• Xie, Y. P.
• Wang, X.
• Wityak, J.
• Karanewsky, D.
• Gerken, A.
• Iskandar, M.
• Saez, Enrique
• Seidel, H. M.
• Tian, S. S.

publication date

• August 2006

journal

• Bioorganic & Medicinal Chemistry Letters  Journal

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.

subject areas

• Amino Acid Motifs
• Animals
• Isoxazoles
• Mice
• Models, Chemical
• PPAR delta
• Receptors, Cytoplasmic and Nuclear
• Transcription Factors
• Transcriptional Activation

Research

keywords

• PPAR delta agonists
• energy homeostasis
• isoxazoles
• metabolic syndrome

Identity

International Standard Serial Number (ISSN)

• 0960-894X

Digital Object Identifier (DOI)

• 10.1016/j.bmcl.2006.05.055

PubMed ID

• 16750626

Additional Document Info

start page

• 4376

end page

• 4380

volume

• 16

issue

• 16