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

Julie Charton; Rebecca Deprez-Poulain; Nathalie Hennuyer; Anne Tailleux; Bart Staels; Benoit Deprez

doi:10.1016/j.bmcl.2008.11.040

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. Epub 2008 Nov 18.

Authors

Julie Charton¹, Rebecca Deprez-Poulain, Nathalie Hennuyer, Anne Tailleux, Bart Staels, Benoit Deprez

Affiliation

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Carboxylic Acids / chemistry*
Oxadiazoles / chemistry*
Receptors, Retinoic Acid / drug effects
Retinoids / chemistry
Retinoids / pharmacology*

Substances

Carboxylic Acids
Oxadiazoles
Receptors, Retinoic Acid
Retinoids
retinoic acid receptor beta