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

Academic Article
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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

  • 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
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Research

keywords

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

International Standard Serial Number (ISSN)

  • 0960-894X

Digital Object Identifier (DOI)

  • 10.1016/j.bmcl.2006.05.055

PubMed ID

  • 16750626
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Additional Document Info

start page

  • 4376

end page

  • 4380

volume

  • 16

issue

  • 16

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