Novel non-carboxylic acid retinoids: 1,2,4-oxadiazol-5-one derivatives

  • Bioorg Med Chem Lett. 2009 Jan 15;19(2):489-92. doi: 10.1016/j.bmcl.2008.11.040.
Julie Charton  1 ,  Rebecca Deprez-Poulain ,  Nathalie Hennuyer ,  Anne Tailleux ,  Bart Staels ,  Benoit Deprez
Affiliations
  • 1. INSERM U761 Biostructures and Drug Discovery, 3 rue du Professeur Laguesse, Lille F-59006, France. [email protected]
PMID: 19058965 DOI: 10.1016/j.bmcl.2008.11.040
Abstract

We have successfully obtained 1,2,4-oxadiazol-5-one bioisoteres of Am580 or Tazarotene-like retinoids. In particular compound 4 displays an EC(50) of 26nM on RAR-beta.